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this.src = '//a.academia-assets.com/images/s200_no_pic.png';" width="200" height="200" src="https://0.academia-photos.com/69159441/17943915/165874500/s200_dr_naglaa.ibrahim.jpg" /></a></div><div class="suggested-user-card__user-info"><a class="suggested-user-card__user-info__header ds2-5-body-sm-bold ds2-5-body-link" href="https://aswu.academia.edu/NaglaaIbrahim">Dr Naglaa Ibrahim</a><p class="suggested-user-card__user-info__subheader ds2-5-body-xs">Aswan University</p></div></div></ul></div><div class="ri-section"><div class="ri-section-header"><span>Interests</span></div><div class="ri-tags-container"><a data-click-track="profile-user-info-expand-research-interests" data-has-card-for-ri-list="17601503" href="https://www.academia.edu/Documents/in/Higher_Education"><div id="js-react-on-rails-context" style="display:none" 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data-props="{"color":"gray","children":["Assessment in Higher Education"]}" data-trace="false" data-dom-id="Pill-react-component-835620d5-60ef-426c-a49d-0a359cc0bb10"></div> <div id="Pill-react-component-835620d5-60ef-426c-a49d-0a359cc0bb10"></div> </a><a data-click-track="profile-user-info-expand-research-interests" data-has-card-for-ri-list="17601503" href="https://www.academia.edu/Documents/in/Higher_Education_Policy"><div class="js-react-on-rails-component" style="display:none" data-component-name="Pill" data-props="{"color":"gray","children":["Higher Education Policy"]}" data-trace="false" data-dom-id="Pill-react-component-d95b4e80-eb03-4222-9faf-20ad6b089309"></div> <div id="Pill-react-component-d95b4e80-eb03-4222-9faf-20ad6b089309"></div> </a></div></div></div></div><div class="right-panel-container"><div class="user-content-wrapper"><div class="uploads-container" id="social-redesign-work-container"><div class="upload-header"><h2 class="ds2-5-heading-sans-serif-xs">Uploads</h2></div><div class="documents-container backbone-social-profile-documents" style="width: 100%;"><div class="u-taCenter"></div><div class="profile--tab_content_container js-tab-pane tab-pane active" id="all"><div class="profile--tab_heading_container js-section-heading" data-section="Papers" id="Papers"><h3 class="profile--tab_heading_container">Papers by Simon Pyke</h3></div><div class="js-work-strip profile--work_container" data-work-id="19876769"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/19876769/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine"><img alt="Research paper thumbnail of Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/19876769/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine">Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/FlowerRobert">Robert Flower</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a></span></div><div class="wp-workCard_item"><span>Journal of Ethnopharmacology</span><span>, 1999</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The antipicornaviral activity of an ethanolic extract of the green aerial parts of the Australian...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The antipicornaviral activity of an ethanolic extract of the green aerial parts of the Australian plant Pterocaulon sphacelatum (Labill.) Benth. &amp;amp;amp;amp; Hook. f. ex F. Muell. has been investigated. This plant has been a favoured traditional medicine, used for the treatment of colds by the Australian Aboriginal people. Antiviral activity-guided fractionation of the extract of P. sphacelatum using an inhibition of poliovirus-induced cytopathic effect assay, has yielded the antiviral flavonoid chrysosplenol C (3,7,3&amp;amp;amp;#39;-trimethoxy-5,6,4&amp;amp;amp;#39;-trihydroxyflavone). This compound is a 4&amp;amp;amp;#39;-hydroxy-3-methoxyflavone, one of a group of compounds known to be potent and specific inhibitors of picornaviral replication. These compounds inhibit the replication of rhinoviruses, the most frequent causative agent of the common cold. The coumarin 6,7,8-trimethoxycoumarin was also isolated from the ethanolic extract.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="19876769"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="19876769"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 19876769; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=19876769]").text(description); $(".js-view-count[data-work-id=19876769]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 19876769; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='19876769']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=19876769]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":19876769,"title":"Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine","internal_url":"https://www.academia.edu/19876769/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine","owner_id":40694093,"coauthors_can_edit":true,"owner":{"id":40694093,"first_name":"Robert","middle_initials":"","last_name":"Flower","page_name":"FlowerRobert","domain_name":"independent","created_at":"2015-12-28T18:15:03.639-08:00","display_name":"Robert Flower","url":"https://independent.academia.edu/FlowerRobert"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="19876747"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/19876747/In_vitro_antiviral_activity_of_the_anthraquinone_chrysophanic_acid_against_poliovirus"><img alt="Research paper thumbnail of In vitro antiviral activity of the anthraquinone chrysophanic acid against poliovirus" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/19876747/In_vitro_antiviral_activity_of_the_anthraquinone_chrysophanic_acid_against_poliovirus">In vitro antiviral activity of the anthraquinone chrysophanic acid against poliovirus</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/FlowerRobert">Robert Flower</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a></span></div><div class="wp-workCard_item"><span>Antiviral Research</span><span>, 2001</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">Chrysophanic acid (1,8-dihydroxy-3-methylanthraquinone), isolated from the Australian Aboriginal ...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">Chrysophanic acid (1,8-dihydroxy-3-methylanthraquinone), isolated from the Australian Aboriginal medicinal plant Dianella longifolia, has been found to inhibit the replication of poliovirus types 2 and 3 (Picornaviridae) in vitro. The compound inhibited poliovirus-induced cytopathic effects in BGM (Buffalo green monkey) kidney cells at a 50% effective concentration of 0.21 and 0.02 microgram/ml for poliovirus types 2 and 3, respectively. The compound inhibited an early stage in the viral replication cycle, but did not have an irreversible virucidal effect on poliovirus particles. Chrysophanic acid did not have significant antiviral activity against five other viruses tested: Coxsackievirus types A21 and B4, human rhinovirus type 2 (Picornaviridae), and the enveloped viruses Ross River virus (Togaviridae) and herpes simplex virus type 1 (Herpesviridae). Four structurally-related anthraquinones--rhein, 1,8-dihydroxyanthraquinone, emodin and aloe-emodin were also tested for activity against poliovirus type 3. None of the four compounds was as active as chrysophanic acid against the virus. The results suggested that two hydrophobic positions on the chrysophanic acid molecule (C-6 and the methyl group attached to C-3) were important for the compound&amp;amp;amp;#39;s activity against poliovirus.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="19876747"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="19876747"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 19876747; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=19876747]").text(description); $(".js-view-count[data-work-id=19876747]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 19876747; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='19876747']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=19876747]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":19876747,"title":"In vitro antiviral activity of the anthraquinone chrysophanic acid against poliovirus","internal_url":"https://www.academia.edu/19876747/In_vitro_antiviral_activity_of_the_anthraquinone_chrysophanic_acid_against_poliovirus","owner_id":40694093,"coauthors_can_edit":true,"owner":{"id":40694093,"first_name":"Robert","middle_initials":"","last_name":"Flower","page_name":"FlowerRobert","domain_name":"independent","created_at":"2015-12-28T18:15:03.639-08:00","display_name":"Robert Flower","url":"https://independent.academia.edu/FlowerRobert"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="17376079"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/17376079/Carbonyl_Scavenging_Drugs_and_Protection_Against_Carbonyl_Stress_Associated_Cell_Injury"><img alt="Research paper thumbnail of Carbonyl-Scavenging Drugs & Protection Against Carbonyl Stress-Associated Cell Injury" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/17376079/Carbonyl_Scavenging_Drugs_and_Protection_Against_Carbonyl_Stress_Associated_Cell_Injury">Carbonyl-Scavenging Drugs & Protection Against Carbonyl Stress-Associated Cell Injury</a></div><div class="wp-workCard_item"><span>Mini-Reviews in Medicinal Chemistry</span><span>, 2008</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">This mini-review highlights the chemical and cytoprotective properties of various hydralazine ana...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">This mini-review highlights the chemical and cytoprotective properties of various hydralazine analogues that block the induction of cell death by acrolein, a highly toxic contributor to &amp;quot;carbonyl stress&amp;quot; during a diverse range of human diseases. Recent work on the action of hydralazine against various carbonyl-mediated pathologies is also reviewed.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="17376079"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="17376079"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 17376079; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=17376079]").text(description); $(".js-view-count[data-work-id=17376079]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 17376079; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='17376079']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=17376079]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":17376079,"title":"Carbonyl-Scavenging Drugs \u0026 Protection Against Carbonyl Stress-Associated Cell Injury","internal_url":"https://www.academia.edu/17376079/Carbonyl_Scavenging_Drugs_and_Protection_Against_Carbonyl_Stress_Associated_Cell_Injury","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="17376078"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/17376078/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine"><img alt="Research paper thumbnail of Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/17376078/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine">Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine</a></div><div class="wp-workCard_item"><span>Journal of Ethnopharmacology</span><span>, 1999</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The antipicornaviral activity of an ethanolic extract of the green aerial parts of the Australian...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The antipicornaviral activity of an ethanolic extract of the green aerial parts of the Australian plant Pterocaulon sphacelatum (Labill.) Benth. &amp;amp;amp;amp; Hook. f. ex F. Muell. has been investigated. This plant has been a favoured traditional medicine, used for the treatment of colds by the Australian Aboriginal people. Antiviral activity-guided fractionation of the extract of P. sphacelatum using an inhibition of poliovirus-induced cytopathic effect assay, has yielded the antiviral flavonoid chrysosplenol C (3,7,3&amp;amp;amp;#39;-trimethoxy-5,6,4&amp;amp;amp;#39;-trihydroxyflavone). This compound is a 4&amp;amp;amp;#39;-hydroxy-3-methoxyflavone, one of a group of compounds known to be potent and specific inhibitors of picornaviral replication. These compounds inhibit the replication of rhinoviruses, the most frequent causative agent of the common cold. The coumarin 6,7,8-trimethoxycoumarin was also isolated from the ethanolic extract.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="17376078"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="17376078"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 17376078; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=17376078]").text(description); $(".js-view-count[data-work-id=17376078]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 17376078; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='17376078']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=17376078]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":17376078,"title":"Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine","internal_url":"https://www.academia.edu/17376078/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="17176262"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/17176262/Identification_and_Specificity_Studies_of_Small_Molecule_Ligands_for_SH3_Protein_Domains"><img alt="Research paper thumbnail of Identification and Specificity Studies of Small-Molecule Ligands for SH3 Protein Domains" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/17176262/Identification_and_Specificity_Studies_of_Small_Molecule_Ligands_for_SH3_Protein_Domains">Identification and Specificity Studies of Small-Molecule Ligands for SH3 Protein Domains</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/KimBranson">Kim Branson</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a></span></div><div class="wp-workCard_item"><span>Journal of Medicinal Chemistry</span><span>, 2004</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The Src Homology 3 (SH3) domains are small protein-protein interaction domains that bind proline-...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The Src Homology 3 (SH3) domains are small protein-protein interaction domains that bind proline-rich sequences and mediate a wide range of cell-signaling and other important biological processes. Since deregulated signaling pathways form the basis of many human diseases, the SH3 domains have been attractive targets for novel therapeutics. High-affinity ligands for SH3 domains have been designed; however, these have all been peptide-based and no examples of entirely nonpeptide SH3 ligands have previously been reported. Using the mouse Tec Kinase SH3 domain as a model system for structure-based ligand design, we have identified several simple heterocyclic compounds that selectively bind to the Tec SH3 domain. Using a combination of nuclear magnetic resonance chemical shift perturbation, structure-activity relationships, and site-directed mutagenesis, the binding of these compounds at the proline-rich peptide-binding site has been characterized. The most potent of these, 2-aminoquinoline, bound with Kd = 125 microM and was able to compete for binding with a proline-rich peptide. Synthesis of 6-substituted-2-aminoquinolines resulted in ligands with up to 6-fold improved affinity over 2-aminoquinoline and enhanced specificity for the Tec SH3 domain. Therefore, 2-aminoquinolines may potentially be useful for the development of high affinity small molecule ligands for SH3 domains.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="17176262"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="17176262"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 17176262; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=17176262]").text(description); 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dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=17176262]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":17176262,"title":"Identification and Specificity Studies of Small-Molecule Ligands for SH3 Protein Domains","internal_url":"https://www.academia.edu/17176262/Identification_and_Specificity_Studies_of_Small_Molecule_Ligands_for_SH3_Protein_Domains","owner_id":36777398,"coauthors_can_edit":true,"owner":{"id":36777398,"first_name":"Kim","middle_initials":null,"last_name":"Branson","page_name":"KimBranson","domain_name":"stanford","created_at":"2015-10-22T15:02:24.586-07:00","display_name":"Kim Branson","url":"https://stanford.academia.edu/KimBranson"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552547"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552547/A_general_method_for_the_preparation_of_single_pendant_arm_2_hydroxyalkyl_1_4_7_triazacyclononane_macrocycles"><img alt="Research paper thumbnail of A general method for the preparation of single pendant arm 2-hydroxyalkyl-1,4,7-triazacyclononane macrocycles" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552547/A_general_method_for_the_preparation_of_single_pendant_arm_2_hydroxyalkyl_1_4_7_triazacyclononane_macrocycles">A general method for the preparation of single pendant arm 2-hydroxyalkyl-1,4,7-triazacyclononane macrocycles</a></div><div class="wp-workCard_item"><span>Journal of The Chemical Society-perkin Transactions 1</span><span>, 1999</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ABSTRACT The facile synthesis of a di-protected 1,4,7-triazacyclononane derivative that provides ...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ABSTRACT The facile synthesis of a di-protected 1,4,7-triazacyclononane derivative that provides a simple route to single pendant arm 2-hydroxyalkyl triaza-macrocycles through reaction with epoxides is described.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552547"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552547"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552547; 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</script> <div class="js-work-strip profile--work_container" data-work-id="8552546"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552546/ChemInform_Abstract_Mechanistic_Investigations_on_the_Reaction_Between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers"><img alt="Research paper thumbnail of ChemInform Abstract: Mechanistic Investigations on the Reaction Between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers" class="work-thumbnail" src="https://attachments.academia-assets.com/48057464/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552546/ChemInform_Abstract_Mechanistic_Investigations_on_the_Reaction_Between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers">ChemInform Abstract: Mechanistic Investigations on the Reaction Between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers</a></div><div class="wp-workCard_item"><span>Cheminform</span><span>, 2010</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="2ab4d538eedcd46c8e7964f88db8acda" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057464,"asset_id":8552546,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057464/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552546"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552546"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552546; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552540"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552540/A_new_method_for_the_synthesis_of_porphyrin_diones_that_is_applicable_to_the_synthesis_of_trans_annular_extended_porphyrin_systems"><img alt="Research paper thumbnail of A new method for the synthesis of porphyrin-?-diones that is applicable to the synthesis of trans-annular extended porphyrin systems" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552540/A_new_method_for_the_synthesis_of_porphyrin_diones_that_is_applicable_to_the_synthesis_of_trans_annular_extended_porphyrin_systems">A new method for the synthesis of porphyrin-?-diones that is applicable to the synthesis of trans-annular extended porphyrin systems</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/ManalRawashdehomary">Manal Rawashdeh-omary</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a></span></div><div class="wp-workCard_item"><span>Journal of The Chemical Society, Chemical Communications</span><span>, 1991</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ABSTRACT Porphyrin-α-diones can be prepared by photooxidation or SeO2-oxidation of β-hydroxyporph...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ABSTRACT Porphyrin-α-diones can be prepared by photooxidation or SeO2-oxidation of β-hydroxyporphyrins, which are in turn readily synthesized from the corresponding copper(II) or nickel(II) 2-halo- and 2-sulphinyl-porphyrins by reaction with the anion of E-benzaldoxime; the efficient conversion of the porphyrinoquinoxaline 6 into the diquinoxalino[2,3-g, 2,3-q] porphyrin 9 illustrates the usefulness of the new methodology for the synthesis of trans-annular extended porphyrin systems.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552540"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552540"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552540; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552540]").text(description); $(".js-view-count[data-work-id=8552540]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552540; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552540']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); 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</script> <div class="js-work-strip profile--work_container" data-work-id="8552539"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552539/Enantioselective_assay_for_the_determination_of_perhexiline_enantiomers_in_human_plasma_by_liquid_chromatography"><img alt="Research paper thumbnail of Enantioselective assay for the determination of perhexiline enantiomers in human plasma by liquid chromatography" class="work-thumbnail" src="https://attachments.academia-assets.com/48057489/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552539/Enantioselective_assay_for_the_determination_of_perhexiline_enantiomers_in_human_plasma_by_liquid_chromatography">Enantioselective assay for the determination of perhexiline enantiomers in human plasma by liquid chromatography</a></div><div class="wp-workCard_item"><span>Journal of Chromatography B-analytical Technologies in The Biomedical and Life Sciences</span><span>, 2006</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">Effective use of the antianginal agent perhexiline is difficult because saturable metabolism by t...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">Effective use of the antianginal agent perhexiline is difficult because saturable metabolism by the polymorphic cytochrome P450 2D6 (CYP2D6) isoform produces elevated plasma perhexiline concentrations that have been associated with serious hepatic and neurological toxicity. Perhexiline is marketed for therapeutic use as a racemate and there is evidence for differences in the disposition of its enantiomers. The current study describes an enantioselective HPLC-fluorescent method utilising pre-column derivatization with (R)-(−)-1-(1-napthyl)ethyl isocyanate. Following derivatization, the enantiomers are resolved on a C18 column with gradient elution using a mobile phase composed of methanol and water. The method described is suitable for the quantification of (+)-and (−)-perhexiline in human plasma following clinical doses and demonstrates sufficient sensitivity, accuracy and precision between 0.01 and 2.00 mg/l for each enantiomer, with intra-assay coefficients of variation and bias <20% at 0.01 mg/l and <10% at 2.00 mg/l, and inter-assay coefficients of variation and biases <15% at 0.03 mg/l and <10% at 0.40 and 0.75 mg/l. The application of this method to plasma samples collected from a patient treated with perhexiline revealed that (+)-perhexiline concentrations were higher than (−)-perhexiline concentrations, confirming the stereoselective disposition of perhexiline. The current study describes an enantioselective method that utilises pre-column formation of fluorescent diastereomers that are resolved on a C18 HPLC column using a gradient of methanol and water.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="d693ef8282ce3fe4a478dfaa722d1e71" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057489,"asset_id":8552539,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057489/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552539"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552539"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552539; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552537"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552537/Synthesis_and_Cyclization_to_Aurones_and_Flavones_of_Alkoxy_Substituted_Aryl_Arylalkynyl_Ketones"><img alt="Research paper thumbnail of Synthesis, and Cyclization to Aurones and Flavones, of Alkoxy-Substituted Aryl, Arylalkynyl Ketones" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552537/Synthesis_and_Cyclization_to_Aurones_and_Flavones_of_Alkoxy_Substituted_Aryl_Arylalkynyl_Ketones">Synthesis, and Cyclization to Aurones and Flavones, of Alkoxy-Substituted Aryl, Arylalkynyl Ketones</a></div><div class="wp-workCard_item"><span>Australian Journal of Chemistry</span><span>, 2008</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552537"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552537"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552537; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552537]").text(description); $(".js-view-count[data-work-id=8552537]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552537; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552537']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=8552537]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552537,"title":"Synthesis, and Cyclization to Aurones and Flavones, of Alkoxy-Substituted Aryl, Arylalkynyl Ketones","internal_url":"https://www.academia.edu/8552537/Synthesis_and_Cyclization_to_Aurones_and_Flavones_of_Alkoxy_Substituted_Aryl_Arylalkynyl_Ketones","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552536"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552536/Mechanistic_Investigations_on_the_Reaction_between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers"><img alt="Research paper thumbnail of Mechanistic Investigations on the Reaction between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552536/Mechanistic_Investigations_on_the_Reaction_between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers">Mechanistic Investigations on the Reaction between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers</a></div><div class="wp-workCard_item"><span>Journal of Organic Chemistry</span><span>, 2001</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The bulky stabilized ylides (2a-d) react with a range of 1,2-dioxines (1a-d) to afford the divers...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The bulky stabilized ylides (2a-d) react with a range of 1,2-dioxines (1a-d) to afford the diversely functionalized cyclopropanes 7 in excellent yield and diastereomeric excess. This is in direct contrast to the situation when nonbulky ester ylides are utilized which results in a completely different cyclopropyl series. Through a combination of isolation, spectroscopic, temperature, and deuterium and additive effects studies, the mechanism of cyclopropane formation from this second pathway can be proposed. Importantly, enolate quenching of the intermediate 1-2lambda(5)-oxaphospholanes 4 prior to collapse results in an equilibrium mixture of intermediates 10 and 11 which have been fully characterized, and their formation is primarily a result of the steric bulk of the stabilized ester ylide. These intermediates (10/11) then collapse further and result in formation of the observed closely related cyclopropyl stereoisomers 7 and 8. Moreover, the addition of LiBr to these reactions allows for the control of which of the two possible cyclopropanation pathways will be dominant. Finally, optimal protocols that demonstrate the potential of this new cyclopropanation methodology for the ready construction of closely related cyclopropyl stereoisomers are presented.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552536"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552536"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552536; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552536]").text(description); $(".js-view-count[data-work-id=8552536]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552536; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552536']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=8552536]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552536,"title":"Mechanistic Investigations on the Reaction between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers","internal_url":"https://www.academia.edu/8552536/Mechanistic_Investigations_on_the_Reaction_between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552535"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552535/Michael_addition_of_acrolein_to_lysinyl_and_N_terminal_residues_of_a_model_peptide_targets_for_cytoprotective_hydrazino_drugs"><img alt="Research paper thumbnail of Michael addition of acrolein to lysinyl and N-terminal residues of a model peptide: targets for cytoprotective hydrazino drugs" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552535/Michael_addition_of_acrolein_to_lysinyl_and_N_terminal_residues_of_a_model_peptide_targets_for_cytoprotective_hydrazino_drugs">Michael addition of acrolein to lysinyl and N-terminal residues of a model peptide: targets for cytoprotective hydrazino drugs</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/PhilipBurcham">Philip Burcham</a></span></div><div class="wp-workCard_item"><span>Rapid Communications in Mass Spectrometry</span><span>, 2007</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The antihypertensive drug hydralazine blocks acrolein-mediated toxicity by trapping both free ald...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The antihypertensive drug hydralazine blocks acrolein-mediated toxicity by trapping both free aldehyde- and acrolein-adducted proteins, with the latter property more closely related to cytoprotection in cellular models. Here we report the identification of products from ‘protein adduct-trapping’ reactions using electrospray ionisation mass spectrometry (ESI-MS). Reaction of a 13-residue peptide containing a single lysine with acrolein for 30 min generated ions corresponding to mono- and bis-Michael-adducted peptides. An ion corresponding to a cyclic species formed from bis-adducted lysine was conspicuous at later times (60, 180 min). Tandem mass spectrometric (MS/MS) analysis revealed Michael adduction also occurred on the N-terminus, with a novel N-terminal (3-formyl-3,4-dehydropiperidino) species formed on this residue. Addition of hydralazine to acrolein-adducted peptides generated a diverse range of hydrazones that were also characterised by MS/MS analysis. The results confirm that mass spectrometry is a powerful tool for characterising the reactions of noxious electrophiles with biological macromolecules. Copyright © 2007 John Wiley & Sons, Ltd.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552535"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552535"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552535; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552535]").text(description); $(".js-view-count[data-work-id=8552535]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552535; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552535']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=8552535]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552535,"title":"Michael addition of acrolein to lysinyl and N-terminal residues of a model peptide: targets for cytoprotective hydrazino drugs","internal_url":"https://www.academia.edu/8552535/Michael_addition_of_acrolein_to_lysinyl_and_N_terminal_residues_of_a_model_peptide_targets_for_cytoprotective_hydrazino_drugs","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552533"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552533/Synthesis_of_N_Benzylated_2_aminoquinolines_as_Ligands_for_the_Tec_SH3_Domain"><img alt="Research paper thumbnail of Synthesis of N-Benzylated-2-aminoquinolines as Ligands for the Tec SH3 Domain" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552533/Synthesis_of_N_Benzylated_2_aminoquinolines_as_Ligands_for_the_Tec_SH3_Domain">Synthesis of N-Benzylated-2-aminoquinolines as Ligands for the Tec SH3 Domain</a></div><div class="wp-workCard_item"><span>Cheminform</span><span>, 2006</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552531"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552531/Complexation_of_Zinc_II_and_Cadmium_II_by_Hydroxyethyl_and_Bis_hydroxyethyl_1_4_7_triazacyclononane_in_Water"><img alt="Research paper thumbnail of Complexation of Zinc(II) and Cadmium(II) by Hydroxyethyl- and Bis(hydroxyethyl)-1,4,7-triazacyclononane in Water" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552531/Complexation_of_Zinc_II_and_Cadmium_II_by_Hydroxyethyl_and_Bis_hydroxyethyl_1_4_7_triazacyclononane_in_Water">Complexation of Zinc(II) and Cadmium(II) by Hydroxyethyl- and Bis(hydroxyethyl)-1,4,7-triazacyclononane in Water</a></div><div class="wp-workCard_item"><span>Australian Journal of Chemistry</span><span>, 2003</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ABSTRACT The complexation of Zn2+ by hydroxyethyl- and bis(hydroxyethyl)-1,4,7-triazacyclononane ...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ABSTRACT The complexation of Zn2+ by hydroxyethyl- and bis(hydroxyethyl)-1,4,7-triazacyclononane ((2) and (3)) in aqueous solution at 298.2 K and I = 0.10 mol dm−3 (NaNO3) is characterized by log(K/dm3 mol−1) = 10.45 ± 0.05 and 11.32 ± 0.02 and a deprotonation assigned to coordinated water is characterized by pKa = 8.87 ± 0.11 and 8.50 ± 0.03, respectively. For the analogous Cd2+ complexes log(K/dm3 mol−1) = 8.74 ± 0.02 and 9.79 ± 0.02, respectively, and no deprotonation of coordinated water is detected. The synthesis of (2) is described.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552531"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552531"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552531; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552531]").text(description); $(".js-view-count[data-work-id=8552531]").attr('title', description).tooltip(); 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</script> <div class="js-work-strip profile--work_container" data-work-id="8552530"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552530/Synthesis_and_characterization_of_triorganotin_IV_complexes_of_5_E_2_aryl_1_diazenyl_2_hydroxybenzoic_acids"><img alt="Research paper thumbnail of Synthesis and characterization of triorganotin(IV) complexes of 5-[( E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoic acids" class="work-thumbnail" src="https://attachments.academia-assets.com/48057494/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552530/Synthesis_and_characterization_of_triorganotin_IV_complexes_of_5_E_2_aryl_1_diazenyl_2_hydroxybenzoic_acids">Synthesis and characterization of triorganotin(IV) complexes of 5-[( E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoic acids</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/TBaul">Tushar Baul</a>, <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a>, and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/RayButcher">Ray Butcher</a></span></div><div class="wp-workCard_item"><span>Journal of Organometallic Chemistry</span><span>, 2001</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The triphenyltin and tri-n-butyltin complexes of some 5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoi...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The triphenyltin and tri-n-butyltin complexes of some 5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoic acids have been synthesized and characterized by 1 H-, 13 C-, 119 Sn-NMR, IR and 119m Sn Mo ¨ssbauer spectroscopic techniques in combination with elemental analysis. The crystal structures of triphenyltin 5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoates (aryl = phenyl, 2-methylphenyl, 3-methylphenyl and 4-methoxyphenyl) are reported. Both X-ray and 119 Sn Mo ¨ssbauer data indicate that the triphenyltin complexes adopt a monomeric distorted tetrahedral configuration with the carboxylate ligand coordinating in a monodentate mode. By contrast, 119 Sn Mo ¨ssbauer spectroscopy shows that each tributyltin complex is polymeric and features a trans-trigonal bipyramidal geometry with a planar SnBu 3 unit and two apical carboxylate oxygen atoms derived from bidentate bridging carboxylate ligands. This is a solid-state effect, as both 119 Sn-NMR and 1 J( 13 C-119/117 Sn) coupling constant data indicate tetrahedral geometries in solution for the triphenyl and tri-n-butyl complexes.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="d61b98449faf593cdf50eaafbe345c1c" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057494,"asset_id":8552530,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057494/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552530"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552530"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552530; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552529"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552529/Sequential_and_Selective_Buchwald_Hartwig_Amination_Reactions_for_the_Controlled_Functionalization_of_6_Bromo_2_chloroquinoline_Synthesis_of_Ligands_for_the_Tec_Src_Homology_3_Domain"><img alt="Research paper thumbnail of Sequential and Selective Buchwald−Hartwig Amination Reactions for the Controlled Functionalization of 6-Bromo-2-chloroquinoline: Synthesis of Ligands for the Tec Src Homology 3 Domain" class="work-thumbnail" src="https://attachments.academia-assets.com/48057467/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552529/Sequential_and_Selective_Buchwald_Hartwig_Amination_Reactions_for_the_Controlled_Functionalization_of_6_Bromo_2_chloroquinoline_Synthesis_of_Ligands_for_the_Tec_Src_Homology_3_Domain">Sequential and Selective Buchwald−Hartwig Amination Reactions for the Controlled Functionalization of 6-Bromo-2-chloroquinoline: Synthesis of Ligands for the Tec Src Homology 3 Domain</a></div><div class="wp-workCard_item"><span>Journal of Organic Chemistry</span><span>, 2008</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">Src homology 3 (SH3) domains are highly conserved protein-protein interaction domains that mediat...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">Src homology 3 (SH3) domains are highly conserved protein-protein interaction domains that mediate important biological processes and are considered valuable targets for the development of therapeutic agents. In this paper, we report the preparation of a range of new 6-heterocyclic substituted 2-aminoquinolines using Buchwald-Hartwig chemistry. 6-Heterocyclic substitution of the 2-aminoquinoline has provided ligands with increased binding affinity for the SH3 domain relative to the lead compound, 2-aminoquinoline, that are the highest affinity ligands prepared to date. The key step in the synthesis of these compounds required a selective Buchwald-Hartwig amination of an aryl bromide in the presence of an activated heteroaryl chloride. The optimization of reaction conditions to achieve the selective amination is discussed and has allowed for cross-coupling with a range of cyclic amines. Introduction of the amino functionality of the 6-heterocyclic 2-aminoquinolines involved additional Buchwald-Hartwig chemistry utilizing lithium bis(trimethylsilyl)amide as an ammonia equivalent. SCHEME 4. Amination of 6 Using LHMDS as an Ammonia Equivalent a a Reaction conditions: 6 (1 equiv), LHMDS (2.2 equiv), Pd2(dba)3 (1 mol %), and 8 (1.2 mol %) in dioxane at 100°C under pressure.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="c8f05628289c5b1e758bf9da26120903" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057467,"asset_id":8552529,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057467/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552529"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552529"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552529; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552528"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552528/Reactivity_with_Tris_hydroxymethyl_aminomethane_Confounds_Immunodetection_of_Acrolein_Adducted_Proteins"><img alt="Research paper thumbnail of Reactivity with Tris(hydroxymethyl)aminomethane Confounds Immunodetection of Acrolein-Adducted Proteins" class="work-thumbnail" src="https://attachments.academia-assets.com/48057475/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552528/Reactivity_with_Tris_hydroxymethyl_aminomethane_Confounds_Immunodetection_of_Acrolein_Adducted_Proteins">Reactivity with Tris(hydroxymethyl)aminomethane Confounds Immunodetection of Acrolein-Adducted Proteins</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a>, <a class="" data-click-track="profile-work-strip-authors" href="https://uq.academia.edu/FrankFontaine">Frank Fontaine</a>, and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/PhilipBurcham">Philip Burcham</a></span></div><div class="wp-workCard_item"><span>Chemical Research in Toxicology</span><span>, 2003</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The toxic R, -unsaturated aldehyde acrolein readily attacks proteins, generating adducts at cyste...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The toxic R, -unsaturated aldehyde acrolein readily attacks proteins, generating adducts at cysteine, histidine, and lysine residues. In this study, rabbit antiserum was raised against acrolein-modified keyhole limpet hemocyanin in the expectation that it would allow immunodetection of adducted proteins in biological samples. Using slot-blot and enzyme-linked immunosorbent assays, the antiserum detected acrolein-modified protein with high sensitivity and specificity. Adduct immunodetection was strongly inhibited by acrolein-modified polylysine but not polyhistidine. Efforts to develop a Western blotting method for detecting adducted proteins in cell lysates were hampered by irreproducible outcomes, evidently due to adduct instability during SDS-PAGE. Indeed, adducts generated via brief exposure of a model protein to acrolein displayed pH-and concentration-dependent instability to tris(hydroxymethyl)aminomethane (Tris), a nucleophilic buffer used in protein electrophoresis. The effect was most striking when Tris solutions were buffered to pH 8.0 and higher. In contrast, adducts formed during extended exposure to acrolein (g60 min) were completely stable to Tris. The time dependence of susceptibility raised the possibility that Tris interfered with specific steps in lysine modification, which involves stepwise Michael addition of two molecules of acrolein to the same residue, followed by condensation and dehydration to form a heterocyclic adduct, N -(3-formyl-3,4-dehydropiperidino)lysine. We hypothesize that carbonyl-retaining Michael adducts may react with Tris by forming imines with the primary amine of the buffer. Consistent with this idea, triethanolamine, a tertiary amine buffer unable to form imines, had no effect on acrolein-adducted protein. These effects of Tris may explain difficulties in the detection of acrolein-adducted proteins during conventional Western blotting procedures.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="c2fcf3eb0d2d169ff964cc89a7bf197c" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057475,"asset_id":8552528,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057475/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552528"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552528"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552528; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552527"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552527/Isolation_of_episulfones_from_the_Ramberg_B_cklund_rearrangement_Part_2_X_Ray_molecular_structure_of_2_3_epithio_8_8_dimethyl_6_10_dioxaspiro_4_5_decane_S_S_dioxide_and_of_r_6_benzyl_t_7_t_8_epithio_1_4_dioxaspiro_4_4_nonane_S_S_dioxide"><img alt="Research paper thumbnail of Isolation of episulfones from the Ramberg?B�cklund rearrangement. Part 2. X-Ray molecular structure of 2,3-epithio-8,8-dimethyl-6,10- dioxaspiro[4.5]decane S,S-dioxide and of r-6-benzyl-t-7,t-8-epithio-1,4-dioxaspiro[4.4]nonane S,S-dioxide" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552527/Isolation_of_episulfones_from_the_Ramberg_B_cklund_rearrangement_Part_2_X_Ray_molecular_structure_of_2_3_epithio_8_8_dimethyl_6_10_dioxaspiro_4_5_decane_S_S_dioxide_and_of_r_6_benzyl_t_7_t_8_epithio_1_4_dioxaspiro_4_4_nonane_S_S_dioxide">Isolation of episulfones from the Ramberg?B�cklund rearrangement. Part 2. X-Ray molecular structure of 2,3-epithio-8,8-dimethyl-6,10- dioxaspiro[4.5]decane S,S-dioxide and of r-6-benzyl-t-7,t-8-epithio-1,4-dioxaspiro[4.4]nonane S,S-dioxide</a></div><div class="wp-workCard_item"><span>Journal of The Chemical Society-perkin Transactions 1</span><span>, 1993</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ABSTRACT For the first time, episulfones have been isolated by the treatment of α-halogeno sulfon...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ABSTRACT For the first time, episulfones have been isolated by the treatment of α-halogeno sulfones with base under the conditions of the Ramberg–Bäcklund reaction. 3,3-Dialkoxy-6-thiabicyclo[3.1.0]hexane dioxides 3a-c and 11a, b have been fully characterised, X-ray crystal structures having been obtained for compounds 3c and 11a. Attempts to prepare episulfones with substituents at the bridgehead position were unsuccessful, however. The thermal stabilities of some of these episulfones have been studied, as have their reactions with base.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552527"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552527"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552527; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552527]").text(description); $(".js-view-count[data-work-id=8552527]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552527; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552527']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=8552527]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552527,"title":"Isolation of episulfones from the Ramberg?B�cklund rearrangement. Part 2. X-Ray molecular structure of 2,3-epithio-8,8-dimethyl-6,10- dioxaspiro[4.5]decane S,S-dioxide and of r-6-benzyl-t-7,t-8-epithio-1,4-dioxaspiro[4.4]nonane S,S-dioxide","internal_url":"https://www.academia.edu/8552527/Isolation_of_episulfones_from_the_Ramberg_B_cklund_rearrangement_Part_2_X_Ray_molecular_structure_of_2_3_epithio_8_8_dimethyl_6_10_dioxaspiro_4_5_decane_S_S_dioxide_and_of_r_6_benzyl_t_7_t_8_epithio_1_4_dioxaspiro_4_4_nonane_S_S_dioxide","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552526"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552526/The_synthesis_characterization_and_structures_of_some_4_E_1_2_hydroxy_5_E_2_aryl_1_diazenyl_phenyl_methylidene_amino_benzoic_acid"><img alt="Research paper thumbnail of The synthesis, characterization and structures of some 4-[(( E)-1-{2-hydroxy-5-[( E)-2-(aryl)-1-diazenyl]phenyl}methylidene)amino]benzoic acid" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552526/The_synthesis_characterization_and_structures_of_some_4_E_1_2_hydroxy_5_E_2_aryl_1_diazenyl_phenyl_methylidene_amino_benzoic_acid">The synthesis, characterization and structures of some 4-[(( E)-1-{2-hydroxy-5-[( E)-2-(aryl)-1-diazenyl]phenyl}methylidene)amino]benzoic acid</a></div><div class="wp-workCard_item"><span>Dyes and Pigments</span><span>, 2009</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The structures of several azo-benzoic acids, 4-[((E)-1-{2-hydroxy-5-[(E)-2-(aryl)-1-diazenyl]phen...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The structures of several azo-benzoic acids, 4-[((E)-1-{2-hydroxy-5-[(E)-2-(aryl)-1-diazenyl]phenyl}methylidene)amino]benzoic acid along with their precursors 2-hydroxy-5-[(E)-(aryldiazenyl)]benzaldehydes were confirmed using 1H, 13C NMR, UV–VIS and IR spectroscopic techniques. UV–VIS absorption spectra were measured in pure organic solvents while complementary spectroscopic experiments using mixed solvent systems as well as in the presence of base were undertaken to characterize the different species present in solution. Both</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552526"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552526"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552526; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552526]").text(description); $(".js-view-count[data-work-id=8552526]").attr('title', description).tooltip(); 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</script> </div><div class="profile--tab_content_container js-tab-pane tab-pane" data-section-id="1895738" id="papers"><div class="js-work-strip profile--work_container" data-work-id="19876769"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/19876769/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine"><img alt="Research paper thumbnail of Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/19876769/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine">Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/FlowerRobert">Robert Flower</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a></span></div><div class="wp-workCard_item"><span>Journal of Ethnopharmacology</span><span>, 1999</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The antipicornaviral activity of an ethanolic extract of the green aerial parts of the Australian...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The antipicornaviral activity of an ethanolic extract of the green aerial parts of the Australian plant Pterocaulon sphacelatum (Labill.) Benth. &amp;amp;amp;amp; Hook. f. ex F. Muell. has been investigated. This plant has been a favoured traditional medicine, used for the treatment of colds by the Australian Aboriginal people. Antiviral activity-guided fractionation of the extract of P. sphacelatum using an inhibition of poliovirus-induced cytopathic effect assay, has yielded the antiviral flavonoid chrysosplenol C (3,7,3&amp;amp;amp;#39;-trimethoxy-5,6,4&amp;amp;amp;#39;-trihydroxyflavone). This compound is a 4&amp;amp;amp;#39;-hydroxy-3-methoxyflavone, one of a group of compounds known to be potent and specific inhibitors of picornaviral replication. These compounds inhibit the replication of rhinoviruses, the most frequent causative agent of the common cold. The coumarin 6,7,8-trimethoxycoumarin was also isolated from the ethanolic extract.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="19876769"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="19876769"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 19876769; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=19876769]").text(description); $(".js-view-count[data-work-id=19876769]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 19876769; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='19876769']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=19876769]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":19876769,"title":"Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine","internal_url":"https://www.academia.edu/19876769/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine","owner_id":40694093,"coauthors_can_edit":true,"owner":{"id":40694093,"first_name":"Robert","middle_initials":"","last_name":"Flower","page_name":"FlowerRobert","domain_name":"independent","created_at":"2015-12-28T18:15:03.639-08:00","display_name":"Robert Flower","url":"https://independent.academia.edu/FlowerRobert"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="19876747"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/19876747/In_vitro_antiviral_activity_of_the_anthraquinone_chrysophanic_acid_against_poliovirus"><img alt="Research paper thumbnail of In vitro antiviral activity of the anthraquinone chrysophanic acid against poliovirus" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/19876747/In_vitro_antiviral_activity_of_the_anthraquinone_chrysophanic_acid_against_poliovirus">In vitro antiviral activity of the anthraquinone chrysophanic acid against poliovirus</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/FlowerRobert">Robert Flower</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a></span></div><div class="wp-workCard_item"><span>Antiviral Research</span><span>, 2001</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">Chrysophanic acid (1,8-dihydroxy-3-methylanthraquinone), isolated from the Australian Aboriginal ...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">Chrysophanic acid (1,8-dihydroxy-3-methylanthraquinone), isolated from the Australian Aboriginal medicinal plant Dianella longifolia, has been found to inhibit the replication of poliovirus types 2 and 3 (Picornaviridae) in vitro. The compound inhibited poliovirus-induced cytopathic effects in BGM (Buffalo green monkey) kidney cells at a 50% effective concentration of 0.21 and 0.02 microgram/ml for poliovirus types 2 and 3, respectively. The compound inhibited an early stage in the viral replication cycle, but did not have an irreversible virucidal effect on poliovirus particles. Chrysophanic acid did not have significant antiviral activity against five other viruses tested: Coxsackievirus types A21 and B4, human rhinovirus type 2 (Picornaviridae), and the enveloped viruses Ross River virus (Togaviridae) and herpes simplex virus type 1 (Herpesviridae). Four structurally-related anthraquinones--rhein, 1,8-dihydroxyanthraquinone, emodin and aloe-emodin were also tested for activity against poliovirus type 3. None of the four compounds was as active as chrysophanic acid against the virus. The results suggested that two hydrophobic positions on the chrysophanic acid molecule (C-6 and the methyl group attached to C-3) were important for the compound&amp;amp;amp;#39;s activity against poliovirus.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="19876747"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="19876747"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 19876747; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); 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dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=19876747]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":19876747,"title":"In vitro antiviral activity of the anthraquinone chrysophanic acid against poliovirus","internal_url":"https://www.academia.edu/19876747/In_vitro_antiviral_activity_of_the_anthraquinone_chrysophanic_acid_against_poliovirus","owner_id":40694093,"coauthors_can_edit":true,"owner":{"id":40694093,"first_name":"Robert","middle_initials":"","last_name":"Flower","page_name":"FlowerRobert","domain_name":"independent","created_at":"2015-12-28T18:15:03.639-08:00","display_name":"Robert Flower","url":"https://independent.academia.edu/FlowerRobert"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="17376079"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/17376079/Carbonyl_Scavenging_Drugs_and_Protection_Against_Carbonyl_Stress_Associated_Cell_Injury"><img alt="Research paper thumbnail of Carbonyl-Scavenging Drugs & Protection Against Carbonyl Stress-Associated Cell Injury" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/17376079/Carbonyl_Scavenging_Drugs_and_Protection_Against_Carbonyl_Stress_Associated_Cell_Injury">Carbonyl-Scavenging Drugs & Protection Against Carbonyl Stress-Associated Cell Injury</a></div><div class="wp-workCard_item"><span>Mini-Reviews in Medicinal Chemistry</span><span>, 2008</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">This mini-review highlights the chemical and cytoprotective properties of various hydralazine ana...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">This mini-review highlights the chemical and cytoprotective properties of various hydralazine analogues that block the induction of cell death by acrolein, a highly toxic contributor to &amp;quot;carbonyl stress&amp;quot; during a diverse range of human diseases. Recent work on the action of hydralazine against various carbonyl-mediated pathologies is also reviewed.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="17376079"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="17376079"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 17376079; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=17376079]").text(description); $(".js-view-count[data-work-id=17376079]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 17376079; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='17376079']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=17376079]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":17376079,"title":"Carbonyl-Scavenging Drugs \u0026 Protection Against Carbonyl Stress-Associated Cell Injury","internal_url":"https://www.academia.edu/17376079/Carbonyl_Scavenging_Drugs_and_Protection_Against_Carbonyl_Stress_Associated_Cell_Injury","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="17376078"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/17376078/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine"><img alt="Research paper thumbnail of Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/17376078/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine">Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine</a></div><div class="wp-workCard_item"><span>Journal of Ethnopharmacology</span><span>, 1999</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The antipicornaviral activity of an ethanolic extract of the green aerial parts of the Australian...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The antipicornaviral activity of an ethanolic extract of the green aerial parts of the Australian plant Pterocaulon sphacelatum (Labill.) Benth. &amp;amp;amp;amp; Hook. f. ex F. Muell. has been investigated. This plant has been a favoured traditional medicine, used for the treatment of colds by the Australian Aboriginal people. Antiviral activity-guided fractionation of the extract of P. sphacelatum using an inhibition of poliovirus-induced cytopathic effect assay, has yielded the antiviral flavonoid chrysosplenol C (3,7,3&amp;amp;amp;#39;-trimethoxy-5,6,4&amp;amp;amp;#39;-trihydroxyflavone). This compound is a 4&amp;amp;amp;#39;-hydroxy-3-methoxyflavone, one of a group of compounds known to be potent and specific inhibitors of picornaviral replication. These compounds inhibit the replication of rhinoviruses, the most frequent causative agent of the common cold. The coumarin 6,7,8-trimethoxycoumarin was also isolated from the ethanolic extract.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="17376078"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="17376078"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 17376078; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=17376078]").text(description); $(".js-view-count[data-work-id=17376078]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 17376078; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='17376078']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=17376078]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":17376078,"title":"Antiviral flavonoid from Pterocaulon sphacelatum, an Australian Aboriginal medicine","internal_url":"https://www.academia.edu/17376078/Antiviral_flavonoid_from_Pterocaulon_sphacelatum_an_Australian_Aboriginal_medicine","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="17176262"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/17176262/Identification_and_Specificity_Studies_of_Small_Molecule_Ligands_for_SH3_Protein_Domains"><img alt="Research paper thumbnail of Identification and Specificity Studies of Small-Molecule Ligands for SH3 Protein Domains" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/17176262/Identification_and_Specificity_Studies_of_Small_Molecule_Ligands_for_SH3_Protein_Domains">Identification and Specificity Studies of Small-Molecule Ligands for SH3 Protein Domains</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/KimBranson">Kim Branson</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a></span></div><div class="wp-workCard_item"><span>Journal of Medicinal Chemistry</span><span>, 2004</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The Src Homology 3 (SH3) domains are small protein-protein interaction domains that bind proline-...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The Src Homology 3 (SH3) domains are small protein-protein interaction domains that bind proline-rich sequences and mediate a wide range of cell-signaling and other important biological processes. Since deregulated signaling pathways form the basis of many human diseases, the SH3 domains have been attractive targets for novel therapeutics. High-affinity ligands for SH3 domains have been designed; however, these have all been peptide-based and no examples of entirely nonpeptide SH3 ligands have previously been reported. Using the mouse Tec Kinase SH3 domain as a model system for structure-based ligand design, we have identified several simple heterocyclic compounds that selectively bind to the Tec SH3 domain. Using a combination of nuclear magnetic resonance chemical shift perturbation, structure-activity relationships, and site-directed mutagenesis, the binding of these compounds at the proline-rich peptide-binding site has been characterized. The most potent of these, 2-aminoquinoline, bound with Kd = 125 microM and was able to compete for binding with a proline-rich peptide. Synthesis of 6-substituted-2-aminoquinolines resulted in ligands with up to 6-fold improved affinity over 2-aminoquinoline and enhanced specificity for the Tec SH3 domain. Therefore, 2-aminoquinolines may potentially be useful for the development of high affinity small molecule ligands for SH3 domains.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="17176262"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="17176262"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 17176262; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=17176262]").text(description); $(".js-view-count[data-work-id=17176262]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 17176262; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='17176262']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=17176262]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":17176262,"title":"Identification and Specificity Studies of Small-Molecule Ligands for SH3 Protein Domains","internal_url":"https://www.academia.edu/17176262/Identification_and_Specificity_Studies_of_Small_Molecule_Ligands_for_SH3_Protein_Domains","owner_id":36777398,"coauthors_can_edit":true,"owner":{"id":36777398,"first_name":"Kim","middle_initials":null,"last_name":"Branson","page_name":"KimBranson","domain_name":"stanford","created_at":"2015-10-22T15:02:24.586-07:00","display_name":"Kim Branson","url":"https://stanford.academia.edu/KimBranson"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552547"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552547/A_general_method_for_the_preparation_of_single_pendant_arm_2_hydroxyalkyl_1_4_7_triazacyclononane_macrocycles"><img alt="Research paper thumbnail of A general method for the preparation of single pendant arm 2-hydroxyalkyl-1,4,7-triazacyclononane macrocycles" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552547/A_general_method_for_the_preparation_of_single_pendant_arm_2_hydroxyalkyl_1_4_7_triazacyclononane_macrocycles">A general method for the preparation of single pendant arm 2-hydroxyalkyl-1,4,7-triazacyclononane macrocycles</a></div><div class="wp-workCard_item"><span>Journal of The Chemical Society-perkin Transactions 1</span><span>, 1999</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ABSTRACT The facile synthesis of a di-protected 1,4,7-triazacyclononane derivative that provides ...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ABSTRACT The facile synthesis of a di-protected 1,4,7-triazacyclononane derivative that provides a simple route to single pendant arm 2-hydroxyalkyl triaza-macrocycles through reaction with epoxides is described.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552547"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552547"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552547; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552547]").text(description); $(".js-view-count[data-work-id=8552547]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552547; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552547']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); 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</script> <div class="js-work-strip profile--work_container" data-work-id="8552546"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552546/ChemInform_Abstract_Mechanistic_Investigations_on_the_Reaction_Between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers"><img alt="Research paper thumbnail of ChemInform Abstract: Mechanistic Investigations on the Reaction Between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers" class="work-thumbnail" src="https://attachments.academia-assets.com/48057464/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552546/ChemInform_Abstract_Mechanistic_Investigations_on_the_Reaction_Between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers">ChemInform Abstract: Mechanistic Investigations on the Reaction Between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers</a></div><div class="wp-workCard_item"><span>Cheminform</span><span>, 2010</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="2ab4d538eedcd46c8e7964f88db8acda" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057464,"asset_id":8552546,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057464/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552546"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552546"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552546; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552546]").text(description); $(".js-view-count[data-work-id=8552546]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552546; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552546']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (true){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552540"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552540/A_new_method_for_the_synthesis_of_porphyrin_diones_that_is_applicable_to_the_synthesis_of_trans_annular_extended_porphyrin_systems"><img alt="Research paper thumbnail of A new method for the synthesis of porphyrin-?-diones that is applicable to the synthesis of trans-annular extended porphyrin systems" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552540/A_new_method_for_the_synthesis_of_porphyrin_diones_that_is_applicable_to_the_synthesis_of_trans_annular_extended_porphyrin_systems">A new method for the synthesis of porphyrin-?-diones that is applicable to the synthesis of trans-annular extended porphyrin systems</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/ManalRawashdehomary">Manal Rawashdeh-omary</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a></span></div><div class="wp-workCard_item"><span>Journal of The Chemical Society, Chemical Communications</span><span>, 1991</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ABSTRACT Porphyrin-α-diones can be prepared by photooxidation or SeO2-oxidation of β-hydroxyporph...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ABSTRACT Porphyrin-α-diones can be prepared by photooxidation or SeO2-oxidation of β-hydroxyporphyrins, which are in turn readily synthesized from the corresponding copper(II) or nickel(II) 2-halo- and 2-sulphinyl-porphyrins by reaction with the anion of E-benzaldoxime; the efficient conversion of the porphyrinoquinoxaline 6 into the diquinoxalino[2,3-g, 2,3-q] porphyrin 9 illustrates the usefulness of the new methodology for the synthesis of trans-annular extended porphyrin systems.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552540"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552540"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552540; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552540]").text(description); $(".js-view-count[data-work-id=8552540]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552540; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552540']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); 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</script> <div class="js-work-strip profile--work_container" data-work-id="8552539"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552539/Enantioselective_assay_for_the_determination_of_perhexiline_enantiomers_in_human_plasma_by_liquid_chromatography"><img alt="Research paper thumbnail of Enantioselective assay for the determination of perhexiline enantiomers in human plasma by liquid chromatography" class="work-thumbnail" src="https://attachments.academia-assets.com/48057489/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552539/Enantioselective_assay_for_the_determination_of_perhexiline_enantiomers_in_human_plasma_by_liquid_chromatography">Enantioselective assay for the determination of perhexiline enantiomers in human plasma by liquid chromatography</a></div><div class="wp-workCard_item"><span>Journal of Chromatography B-analytical Technologies in The Biomedical and Life Sciences</span><span>, 2006</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">Effective use of the antianginal agent perhexiline is difficult because saturable metabolism by t...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">Effective use of the antianginal agent perhexiline is difficult because saturable metabolism by the polymorphic cytochrome P450 2D6 (CYP2D6) isoform produces elevated plasma perhexiline concentrations that have been associated with serious hepatic and neurological toxicity. Perhexiline is marketed for therapeutic use as a racemate and there is evidence for differences in the disposition of its enantiomers. The current study describes an enantioselective HPLC-fluorescent method utilising pre-column derivatization with (R)-(−)-1-(1-napthyl)ethyl isocyanate. Following derivatization, the enantiomers are resolved on a C18 column with gradient elution using a mobile phase composed of methanol and water. The method described is suitable for the quantification of (+)-and (−)-perhexiline in human plasma following clinical doses and demonstrates sufficient sensitivity, accuracy and precision between 0.01 and 2.00 mg/l for each enantiomer, with intra-assay coefficients of variation and bias <20% at 0.01 mg/l and <10% at 2.00 mg/l, and inter-assay coefficients of variation and biases <15% at 0.03 mg/l and <10% at 0.40 and 0.75 mg/l. The application of this method to plasma samples collected from a patient treated with perhexiline revealed that (+)-perhexiline concentrations were higher than (−)-perhexiline concentrations, confirming the stereoselective disposition of perhexiline. The current study describes an enantioselective method that utilises pre-column formation of fluorescent diastereomers that are resolved on a C18 HPLC column using a gradient of methanol and water.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="d693ef8282ce3fe4a478dfaa722d1e71" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057489,"asset_id":8552539,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057489/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552539"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552539"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552539; 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dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "d693ef8282ce3fe4a478dfaa722d1e71" } } $('.js-work-strip[data-work-id=8552539]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552539,"title":"Enantioselective assay for the determination of perhexiline enantiomers in human plasma by liquid chromatography","internal_url":"https://www.academia.edu/8552539/Enantioselective_assay_for_the_determination_of_perhexiline_enantiomers_in_human_plasma_by_liquid_chromatography","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[{"id":48057489,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/48057489/thumbnails/1.jpg","file_name":"j.jchromb.2005.12.04620160814-8868-10pdj5v.pdf","download_url":"https://www.academia.edu/attachments/48057489/download_file","bulk_download_file_name":"Enantioselective_assay_for_the_determina.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/48057489/j.jchromb.2005.12.04620160814-8868-10pdj5v-libre.pdf?1471239482=\u0026response-content-disposition=attachment%3B+filename%3DEnantioselective_assay_for_the_determina.pdf\u0026Expires=1740276350\u0026Signature=OyL1r9k9CyXkHWZGrIx2OjzKu2SkKq~5cuabjoIENplNFUAkR7G2JJbUGAIDN1DwEy3EcUiR0ku~mt~LQG3f4TsaYYn6jsb~tS1dGBnjoa1PR5ieEB1TlWswUKcVbEzBxz1kzo-n8XAmLtOK3XEh7bPIU1bihqIlcMDBH08r5KM8j3of6a8aAdZ6RV0Udn3S17pMauGlzsj8WGACTmSej3kWXtlgzJwLnV6dW3OFHi9PQtjl7nUqZ49fjq~PEl95-jToUsfztsSPTeZnC~Kq575GHmGM-0si~zw-zcCcIDXajn051aPxckd45mHO8uTOtJEWgWnyCTs6ISLx0TBT6Q__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552537"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552537/Synthesis_and_Cyclization_to_Aurones_and_Flavones_of_Alkoxy_Substituted_Aryl_Arylalkynyl_Ketones"><img alt="Research paper thumbnail of Synthesis, and Cyclization to Aurones and Flavones, of Alkoxy-Substituted Aryl, Arylalkynyl Ketones" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552537/Synthesis_and_Cyclization_to_Aurones_and_Flavones_of_Alkoxy_Substituted_Aryl_Arylalkynyl_Ketones">Synthesis, and Cyclization to Aurones and Flavones, of Alkoxy-Substituted Aryl, Arylalkynyl Ketones</a></div><div class="wp-workCard_item"><span>Australian Journal of Chemistry</span><span>, 2008</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552537"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552537"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552537; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552537]").text(description); $(".js-view-count[data-work-id=8552537]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552537; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552537']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=8552537]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552537,"title":"Synthesis, and Cyclization to Aurones and Flavones, of Alkoxy-Substituted Aryl, Arylalkynyl Ketones","internal_url":"https://www.academia.edu/8552537/Synthesis_and_Cyclization_to_Aurones_and_Flavones_of_Alkoxy_Substituted_Aryl_Arylalkynyl_Ketones","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552536"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552536/Mechanistic_Investigations_on_the_Reaction_between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers"><img alt="Research paper thumbnail of Mechanistic Investigations on the Reaction between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552536/Mechanistic_Investigations_on_the_Reaction_between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers">Mechanistic Investigations on the Reaction between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers</a></div><div class="wp-workCard_item"><span>Journal of Organic Chemistry</span><span>, 2001</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The bulky stabilized ylides (2a-d) react with a range of 1,2-dioxines (1a-d) to afford the divers...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The bulky stabilized ylides (2a-d) react with a range of 1,2-dioxines (1a-d) to afford the diversely functionalized cyclopropanes 7 in excellent yield and diastereomeric excess. This is in direct contrast to the situation when nonbulky ester ylides are utilized which results in a completely different cyclopropyl series. Through a combination of isolation, spectroscopic, temperature, and deuterium and additive effects studies, the mechanism of cyclopropane formation from this second pathway can be proposed. Importantly, enolate quenching of the intermediate 1-2lambda(5)-oxaphospholanes 4 prior to collapse results in an equilibrium mixture of intermediates 10 and 11 which have been fully characterized, and their formation is primarily a result of the steric bulk of the stabilized ester ylide. These intermediates (10/11) then collapse further and result in formation of the observed closely related cyclopropyl stereoisomers 7 and 8. Moreover, the addition of LiBr to these reactions allows for the control of which of the two possible cyclopropanation pathways will be dominant. Finally, optimal protocols that demonstrate the potential of this new cyclopropanation methodology for the ready construction of closely related cyclopropyl stereoisomers are presented.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552536"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552536"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552536; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552536]").text(description); $(".js-view-count[data-work-id=8552536]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552536; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552536']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=8552536]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552536,"title":"Mechanistic Investigations on the Reaction between 1,2-Dioxines and Bulky Stabilized Phosphorus Ylides: An Efficient Route to Closely Related Cyclopropane Stereoisomers","internal_url":"https://www.academia.edu/8552536/Mechanistic_Investigations_on_the_Reaction_between_1_2_Dioxines_and_Bulky_Stabilized_Phosphorus_Ylides_An_Efficient_Route_to_Closely_Related_Cyclopropane_Stereoisomers","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552535"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552535/Michael_addition_of_acrolein_to_lysinyl_and_N_terminal_residues_of_a_model_peptide_targets_for_cytoprotective_hydrazino_drugs"><img alt="Research paper thumbnail of Michael addition of acrolein to lysinyl and N-terminal residues of a model peptide: targets for cytoprotective hydrazino drugs" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552535/Michael_addition_of_acrolein_to_lysinyl_and_N_terminal_residues_of_a_model_peptide_targets_for_cytoprotective_hydrazino_drugs">Michael addition of acrolein to lysinyl and N-terminal residues of a model peptide: targets for cytoprotective hydrazino drugs</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/PhilipBurcham">Philip Burcham</a></span></div><div class="wp-workCard_item"><span>Rapid Communications in Mass Spectrometry</span><span>, 2007</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The antihypertensive drug hydralazine blocks acrolein-mediated toxicity by trapping both free ald...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The antihypertensive drug hydralazine blocks acrolein-mediated toxicity by trapping both free aldehyde- and acrolein-adducted proteins, with the latter property more closely related to cytoprotection in cellular models. Here we report the identification of products from ‘protein adduct-trapping’ reactions using electrospray ionisation mass spectrometry (ESI-MS). Reaction of a 13-residue peptide containing a single lysine with acrolein for 30 min generated ions corresponding to mono- and bis-Michael-adducted peptides. An ion corresponding to a cyclic species formed from bis-adducted lysine was conspicuous at later times (60, 180 min). Tandem mass spectrometric (MS/MS) analysis revealed Michael adduction also occurred on the N-terminus, with a novel N-terminal (3-formyl-3,4-dehydropiperidino) species formed on this residue. Addition of hydralazine to acrolein-adducted peptides generated a diverse range of hydrazones that were also characterised by MS/MS analysis. The results confirm that mass spectrometry is a powerful tool for characterising the reactions of noxious electrophiles with biological macromolecules. Copyright © 2007 John Wiley & Sons, Ltd.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552535"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552535"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552535; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552535]").text(description); $(".js-view-count[data-work-id=8552535]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552535; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552535']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=8552535]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552535,"title":"Michael addition of acrolein to lysinyl and N-terminal residues of a model peptide: targets for cytoprotective hydrazino drugs","internal_url":"https://www.academia.edu/8552535/Michael_addition_of_acrolein_to_lysinyl_and_N_terminal_residues_of_a_model_peptide_targets_for_cytoprotective_hydrazino_drugs","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552533"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552533/Synthesis_of_N_Benzylated_2_aminoquinolines_as_Ligands_for_the_Tec_SH3_Domain"><img alt="Research paper thumbnail of Synthesis of N-Benzylated-2-aminoquinolines as Ligands for the Tec SH3 Domain" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552533/Synthesis_of_N_Benzylated_2_aminoquinolines_as_Ligands_for_the_Tec_SH3_Domain">Synthesis of N-Benzylated-2-aminoquinolines as Ligands for the Tec SH3 Domain</a></div><div class="wp-workCard_item"><span>Cheminform</span><span>, 2006</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552533"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552533"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552533; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552533]").text(description); $(".js-view-count[data-work-id=8552533]").attr('title', description).tooltip(); 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552531"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552531/Complexation_of_Zinc_II_and_Cadmium_II_by_Hydroxyethyl_and_Bis_hydroxyethyl_1_4_7_triazacyclononane_in_Water"><img alt="Research paper thumbnail of Complexation of Zinc(II) and Cadmium(II) by Hydroxyethyl- and Bis(hydroxyethyl)-1,4,7-triazacyclononane in Water" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552531/Complexation_of_Zinc_II_and_Cadmium_II_by_Hydroxyethyl_and_Bis_hydroxyethyl_1_4_7_triazacyclononane_in_Water">Complexation of Zinc(II) and Cadmium(II) by Hydroxyethyl- and Bis(hydroxyethyl)-1,4,7-triazacyclononane in Water</a></div><div class="wp-workCard_item"><span>Australian Journal of Chemistry</span><span>, 2003</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ABSTRACT The complexation of Zn2+ by hydroxyethyl- and bis(hydroxyethyl)-1,4,7-triazacyclononane ...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ABSTRACT The complexation of Zn2+ by hydroxyethyl- and bis(hydroxyethyl)-1,4,7-triazacyclononane ((2) and (3)) in aqueous solution at 298.2 K and I = 0.10 mol dm−3 (NaNO3) is characterized by log(K/dm3 mol−1) = 10.45 ± 0.05 and 11.32 ± 0.02 and a deprotonation assigned to coordinated water is characterized by pKa = 8.87 ± 0.11 and 8.50 ± 0.03, respectively. For the analogous Cd2+ complexes log(K/dm3 mol−1) = 8.74 ± 0.02 and 9.79 ± 0.02, respectively, and no deprotonation of coordinated water is detected. The synthesis of (2) is described.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552531"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552531"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552531; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552531]").text(description); $(".js-view-count[data-work-id=8552531]").attr('title', description).tooltip(); 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</script> <div class="js-work-strip profile--work_container" data-work-id="8552530"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552530/Synthesis_and_characterization_of_triorganotin_IV_complexes_of_5_E_2_aryl_1_diazenyl_2_hydroxybenzoic_acids"><img alt="Research paper thumbnail of Synthesis and characterization of triorganotin(IV) complexes of 5-[( E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoic acids" class="work-thumbnail" src="https://attachments.academia-assets.com/48057494/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552530/Synthesis_and_characterization_of_triorganotin_IV_complexes_of_5_E_2_aryl_1_diazenyl_2_hydroxybenzoic_acids">Synthesis and characterization of triorganotin(IV) complexes of 5-[( E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoic acids</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/TBaul">Tushar Baul</a>, <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a>, and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/RayButcher">Ray Butcher</a></span></div><div class="wp-workCard_item"><span>Journal of Organometallic Chemistry</span><span>, 2001</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The triphenyltin and tri-n-butyltin complexes of some 5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoi...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The triphenyltin and tri-n-butyltin complexes of some 5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoic acids have been synthesized and characterized by 1 H-, 13 C-, 119 Sn-NMR, IR and 119m Sn Mo ¨ssbauer spectroscopic techniques in combination with elemental analysis. The crystal structures of triphenyltin 5-[(E)-2-(aryl)-1-diazenyl]-2-hydroxybenzoates (aryl = phenyl, 2-methylphenyl, 3-methylphenyl and 4-methoxyphenyl) are reported. Both X-ray and 119 Sn Mo ¨ssbauer data indicate that the triphenyltin complexes adopt a monomeric distorted tetrahedral configuration with the carboxylate ligand coordinating in a monodentate mode. By contrast, 119 Sn Mo ¨ssbauer spectroscopy shows that each tributyltin complex is polymeric and features a trans-trigonal bipyramidal geometry with a planar SnBu 3 unit and two apical carboxylate oxygen atoms derived from bidentate bridging carboxylate ligands. This is a solid-state effect, as both 119 Sn-NMR and 1 J( 13 C-119/117 Sn) coupling constant data indicate tetrahedral geometries in solution for the triphenyl and tri-n-butyl complexes.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="d61b98449faf593cdf50eaafbe345c1c" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057494,"asset_id":8552530,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057494/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552530"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552530"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552530; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552529"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552529/Sequential_and_Selective_Buchwald_Hartwig_Amination_Reactions_for_the_Controlled_Functionalization_of_6_Bromo_2_chloroquinoline_Synthesis_of_Ligands_for_the_Tec_Src_Homology_3_Domain"><img alt="Research paper thumbnail of Sequential and Selective Buchwald−Hartwig Amination Reactions for the Controlled Functionalization of 6-Bromo-2-chloroquinoline: Synthesis of Ligands for the Tec Src Homology 3 Domain" class="work-thumbnail" src="https://attachments.academia-assets.com/48057467/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552529/Sequential_and_Selective_Buchwald_Hartwig_Amination_Reactions_for_the_Controlled_Functionalization_of_6_Bromo_2_chloroquinoline_Synthesis_of_Ligands_for_the_Tec_Src_Homology_3_Domain">Sequential and Selective Buchwald−Hartwig Amination Reactions for the Controlled Functionalization of 6-Bromo-2-chloroquinoline: Synthesis of Ligands for the Tec Src Homology 3 Domain</a></div><div class="wp-workCard_item"><span>Journal of Organic Chemistry</span><span>, 2008</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">Src homology 3 (SH3) domains are highly conserved protein-protein interaction domains that mediat...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">Src homology 3 (SH3) domains are highly conserved protein-protein interaction domains that mediate important biological processes and are considered valuable targets for the development of therapeutic agents. In this paper, we report the preparation of a range of new 6-heterocyclic substituted 2-aminoquinolines using Buchwald-Hartwig chemistry. 6-Heterocyclic substitution of the 2-aminoquinoline has provided ligands with increased binding affinity for the SH3 domain relative to the lead compound, 2-aminoquinoline, that are the highest affinity ligands prepared to date. The key step in the synthesis of these compounds required a selective Buchwald-Hartwig amination of an aryl bromide in the presence of an activated heteroaryl chloride. The optimization of reaction conditions to achieve the selective amination is discussed and has allowed for cross-coupling with a range of cyclic amines. Introduction of the amino functionality of the 6-heterocyclic 2-aminoquinolines involved additional Buchwald-Hartwig chemistry utilizing lithium bis(trimethylsilyl)amide as an ammonia equivalent. SCHEME 4. Amination of 6 Using LHMDS as an Ammonia Equivalent a a Reaction conditions: 6 (1 equiv), LHMDS (2.2 equiv), Pd2(dba)3 (1 mol %), and 8 (1.2 mol %) in dioxane at 100°C under pressure.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="c8f05628289c5b1e758bf9da26120903" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057467,"asset_id":8552529,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057467/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552529"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552529"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552529; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552528"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/8552528/Reactivity_with_Tris_hydroxymethyl_aminomethane_Confounds_Immunodetection_of_Acrolein_Adducted_Proteins"><img alt="Research paper thumbnail of Reactivity with Tris(hydroxymethyl)aminomethane Confounds Immunodetection of Acrolein-Adducted Proteins" class="work-thumbnail" src="https://attachments.academia-assets.com/48057475/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/8552528/Reactivity_with_Tris_hydroxymethyl_aminomethane_Confounds_Immunodetection_of_Acrolein_Adducted_Proteins">Reactivity with Tris(hydroxymethyl)aminomethane Confounds Immunodetection of Acrolein-Adducted Proteins</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SimonPyke">Simon Pyke</a>, <a class="" data-click-track="profile-work-strip-authors" href="https://uq.academia.edu/FrankFontaine">Frank Fontaine</a>, and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/PhilipBurcham">Philip Burcham</a></span></div><div class="wp-workCard_item"><span>Chemical Research in Toxicology</span><span>, 2003</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The toxic R, -unsaturated aldehyde acrolein readily attacks proteins, generating adducts at cyste...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The toxic R, -unsaturated aldehyde acrolein readily attacks proteins, generating adducts at cysteine, histidine, and lysine residues. In this study, rabbit antiserum was raised against acrolein-modified keyhole limpet hemocyanin in the expectation that it would allow immunodetection of adducted proteins in biological samples. Using slot-blot and enzyme-linked immunosorbent assays, the antiserum detected acrolein-modified protein with high sensitivity and specificity. Adduct immunodetection was strongly inhibited by acrolein-modified polylysine but not polyhistidine. Efforts to develop a Western blotting method for detecting adducted proteins in cell lysates were hampered by irreproducible outcomes, evidently due to adduct instability during SDS-PAGE. Indeed, adducts generated via brief exposure of a model protein to acrolein displayed pH-and concentration-dependent instability to tris(hydroxymethyl)aminomethane (Tris), a nucleophilic buffer used in protein electrophoresis. The effect was most striking when Tris solutions were buffered to pH 8.0 and higher. In contrast, adducts formed during extended exposure to acrolein (g60 min) were completely stable to Tris. The time dependence of susceptibility raised the possibility that Tris interfered with specific steps in lysine modification, which involves stepwise Michael addition of two molecules of acrolein to the same residue, followed by condensation and dehydration to form a heterocyclic adduct, N -(3-formyl-3,4-dehydropiperidino)lysine. We hypothesize that carbonyl-retaining Michael adducts may react with Tris by forming imines with the primary amine of the buffer. Consistent with this idea, triethanolamine, a tertiary amine buffer unable to form imines, had no effect on acrolein-adducted protein. These effects of Tris may explain difficulties in the detection of acrolein-adducted proteins during conventional Western blotting procedures.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="c2fcf3eb0d2d169ff964cc89a7bf197c" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":48057475,"asset_id":8552528,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/48057475/download_file?s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552528"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552528"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552528; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552527"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552527/Isolation_of_episulfones_from_the_Ramberg_B_cklund_rearrangement_Part_2_X_Ray_molecular_structure_of_2_3_epithio_8_8_dimethyl_6_10_dioxaspiro_4_5_decane_S_S_dioxide_and_of_r_6_benzyl_t_7_t_8_epithio_1_4_dioxaspiro_4_4_nonane_S_S_dioxide"><img alt="Research paper thumbnail of Isolation of episulfones from the Ramberg?B�cklund rearrangement. Part 2. X-Ray molecular structure of 2,3-epithio-8,8-dimethyl-6,10- dioxaspiro[4.5]decane S,S-dioxide and of r-6-benzyl-t-7,t-8-epithio-1,4-dioxaspiro[4.4]nonane S,S-dioxide" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552527/Isolation_of_episulfones_from_the_Ramberg_B_cklund_rearrangement_Part_2_X_Ray_molecular_structure_of_2_3_epithio_8_8_dimethyl_6_10_dioxaspiro_4_5_decane_S_S_dioxide_and_of_r_6_benzyl_t_7_t_8_epithio_1_4_dioxaspiro_4_4_nonane_S_S_dioxide">Isolation of episulfones from the Ramberg?B�cklund rearrangement. Part 2. X-Ray molecular structure of 2,3-epithio-8,8-dimethyl-6,10- dioxaspiro[4.5]decane S,S-dioxide and of r-6-benzyl-t-7,t-8-epithio-1,4-dioxaspiro[4.4]nonane S,S-dioxide</a></div><div class="wp-workCard_item"><span>Journal of The Chemical Society-perkin Transactions 1</span><span>, 1993</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">ABSTRACT For the first time, episulfones have been isolated by the treatment of α-halogeno sulfon...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">ABSTRACT For the first time, episulfones have been isolated by the treatment of α-halogeno sulfones with base under the conditions of the Ramberg–Bäcklund reaction. 3,3-Dialkoxy-6-thiabicyclo[3.1.0]hexane dioxides 3a-c and 11a, b have been fully characterised, X-ray crystal structures having been obtained for compounds 3c and 11a. Attempts to prepare episulfones with substituents at the bridgehead position were unsuccessful, however. The thermal stabilities of some of these episulfones have been studied, as have their reactions with base.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552527"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552527"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552527; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552527]").text(description); $(".js-view-count[data-work-id=8552527]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 8552527; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='8552527']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-a9bf3a2bc8c89fa2a77156577594264ee8a0f214d74241bc0fcd3f69f8d107ac.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (false){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "-1" } } $('.js-work-strip[data-work-id=8552527]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":8552527,"title":"Isolation of episulfones from the Ramberg?B�cklund rearrangement. Part 2. X-Ray molecular structure of 2,3-epithio-8,8-dimethyl-6,10- dioxaspiro[4.5]decane S,S-dioxide and of r-6-benzyl-t-7,t-8-epithio-1,4-dioxaspiro[4.4]nonane S,S-dioxide","internal_url":"https://www.academia.edu/8552527/Isolation_of_episulfones_from_the_Ramberg_B_cklund_rearrangement_Part_2_X_Ray_molecular_structure_of_2_3_epithio_8_8_dimethyl_6_10_dioxaspiro_4_5_decane_S_S_dioxide_and_of_r_6_benzyl_t_7_t_8_epithio_1_4_dioxaspiro_4_4_nonane_S_S_dioxide","owner_id":17601503,"coauthors_can_edit":true,"owner":{"id":17601503,"first_name":"Simon","middle_initials":null,"last_name":"Pyke","page_name":"SimonPyke","domain_name":"independent","created_at":"2014-09-29T08:58:16.374-07:00","display_name":"Simon Pyke","url":"https://independent.academia.edu/SimonPyke"},"attachments":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="8552526"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" rel="nofollow" href="https://www.academia.edu/8552526/The_synthesis_characterization_and_structures_of_some_4_E_1_2_hydroxy_5_E_2_aryl_1_diazenyl_phenyl_methylidene_amino_benzoic_acid"><img alt="Research paper thumbnail of The synthesis, characterization and structures of some 4-[(( E)-1-{2-hydroxy-5-[( E)-2-(aryl)-1-diazenyl]phenyl}methylidene)amino]benzoic acid" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" rel="nofollow" href="https://www.academia.edu/8552526/The_synthesis_characterization_and_structures_of_some_4_E_1_2_hydroxy_5_E_2_aryl_1_diazenyl_phenyl_methylidene_amino_benzoic_acid">The synthesis, characterization and structures of some 4-[(( E)-1-{2-hydroxy-5-[( E)-2-(aryl)-1-diazenyl]phenyl}methylidene)amino]benzoic acid</a></div><div class="wp-workCard_item"><span>Dyes and Pigments</span><span>, 2009</span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">The structures of several azo-benzoic acids, 4-[((E)-1-{2-hydroxy-5-[(E)-2-(aryl)-1-diazenyl]phen...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">The structures of several azo-benzoic acids, 4-[((E)-1-{2-hydroxy-5-[(E)-2-(aryl)-1-diazenyl]phenyl}methylidene)amino]benzoic acid along with their precursors 2-hydroxy-5-[(E)-(aryldiazenyl)]benzaldehydes were confirmed using 1H, 13C NMR, UV–VIS and IR spectroscopic techniques. UV–VIS absorption spectra were measured in pure organic solvents while complementary spectroscopic experiments using mixed solvent systems as well as in the presence of base were undertaken to characterize the different species present in solution. Both</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="8552526"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="8552526"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 8552526; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=8552526]").text(description); $(".js-view-count[data-work-id=8552526]").attr('title', description).tooltip(); 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