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dc.contributor.authorWilkinson, Brendanen_US
dc.contributor.authorBornaghi, Laurenten_US
dc.contributor.authorHouston, Todden_US
dc.contributor.authorInnocenti, Alessioen_US
dc.contributor.authorT. Supuran, Claudiuen_US
dc.contributor.authorPoulsen, Sally-Annen_US
dc.contributor.editorPhilip S. Portogheseen_US
dc.date.accessioned2017-04-24T08:40:31Z
dc.date.available2017-04-24T08:40:31Z
dc.date.issued2006en_US
dc.date.modified2009-12-02T05:54:05Z
dc.identifier.issn0022-2623en_US
dc.identifier.doi10.1021/jm060967zen_AU
dc.identifier.urihttp://hdl.handle.net/10072/11308
dc.description.abstractAryl and heteroaryl sulfonamides (ArSO2NH2) are therapeutically used to inhibit the catalytic activity of carbonic anhydrases (CAs). Using a "click-tail" approach a novel class of glycoconjugate benzene sulfonamides have been synthesized that contain diverse carbohydrate-triazole tails. These compounds were assessed for their ability to inhibit three human CA isozymes in vitro: cytosolic hCA I and hCA II and transmembrane, tumor-associated hCA IX. This isozyme has a minimal expression in normal tissue but is overexpressed in hypoxic tumors and its inhibition is a current approach toward new cancer therapies. The qualitative structure-activity for all derivatives demonstrated that the stereochemical diversity present within the carbohydrate tails effectively interrogated the CA active site topology, to generate several inhibitors that were potent and selective toward hCA IX, an important outcome in the quest for potential cancer therapy applications based on CA inhibition.en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_AU
dc.format.extent454813 bytes
dc.format.mimetypeapplication/pdf
dc.languageEnglishen_US
dc.language.isoen_AU
dc.publisherAmerican Chemical Societyen_US
dc.publisher.placeColumbus, Ohioen_US
dc.publisher.urihttp://pubs.acs.org/journal/jmcmar?cookieSet=1en_AU
dc.relation.ispartofstudentpublicationYen_AU
dc.relation.ispartofpagefrom6539en_US
dc.relation.ispartofpageto6548en_US
dc.relation.ispartofedition2006en_US
dc.relation.ispartofissue22en_US
dc.relation.ispartofjournalJournal of Medicinal Chemistryen_US
dc.relation.ispartofvolume49en_US
dc.rights.retentionNen_AU
dc.subject.fieldofresearchcode250302en_US
dc.titleA novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing"en_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.facultyGriffith Sciences, School of Natural Sciencesen_US
gro.rights.copyrightCopyright 2006 American Chemical Society. Self-archiving of the author-manuscript version is not yet supported by this publisher. Please use the hypertext link to access the journal's website or contact the author for more information. Please refer to the journal for the definitive published version.en_AU
gro.date.issued2006
gro.hasfulltextFull Text


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