Please use this identifier to cite or link to this item:
https://hdl.handle.net/1959.11/22910
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DC Field | Value | Language |
---|---|---|
dc.contributor.author | Wilkinson, Brendan | en |
dc.contributor.author | Bornaghi, Laurent F | en |
dc.contributor.author | Houston, Todd A | en |
dc.contributor.author | Innocenti, Alessio | en |
dc.contributor.author | Supuran, Claudiu T | en |
dc.contributor.author | Poulsen, Sally-Ann | en |
dc.date.accessioned | 2018-04-27T13:51:00Z | - |
dc.date.issued | 2006 | - |
dc.identifier.citation | Journal of Medicinal Chemistry, 49(22), p. 6539-6548 | en |
dc.identifier.issn | 1520-4804 | en |
dc.identifier.issn | 0022-2623 | en |
dc.identifier.uri | https://hdl.handle.net/1959.11/22910 | - |
dc.description.abstract | Aryl 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 |
dc.language | en | en |
dc.publisher | American Chemical Society | en |
dc.relation.ispartof | Journal of Medicinal Chemistry | en |
dc.title | A Novel Class of Carbonic Anhydrase Inhibitors: Glycoconjugate Benzene Sulfonamides Prepared by "Click-Tailing" | en |
dc.type | Journal Article | en |
dc.identifier.doi | 10.1021/jm060967z | en |
dc.subject.keywords | Medicinal and Biomolecular Chemistry | en |
dc.subject.keywords | Organic Green Chemistry | en |
dc.subject.keywords | Biologically Active Molecules | en |
local.contributor.firstname | Brendan | en |
local.contributor.firstname | Laurent F | en |
local.contributor.firstname | Todd A | en |
local.contributor.firstname | Alessio | en |
local.contributor.firstname | Claudiu T | en |
local.contributor.firstname | Sally-Ann | en |
local.subject.for2008 | 030499 Medicinal and Biomolecular Chemistry not elsewhere classified | en |
local.subject.for2008 | 030504 Organic Green Chemistry | en |
local.subject.for2008 | 030401 Biologically Active Molecules | en |
local.subject.seo2008 | 970106 Expanding Knowledge in the Biological Sciences | en |
local.subject.seo2008 | 929999 Health not elsewhere classified | en |
local.subject.seo2008 | 970103 Expanding Knowledge in the Chemical Sciences | en |
local.profile.school | School of Science and Technology | en |
local.profile.email | bwilkin7@une.edu.au | en |
local.output.category | C1 | en |
local.record.place | au | en |
local.record.institution | University of New England | en |
local.identifier.epublicationsrecord | une-20180425-102438 | en |
local.publisher.place | United States of America | en |
local.format.startpage | 6539 | en |
local.format.endpage | 6548 | en |
local.identifier.scopusid | 33750471952 | en |
local.peerreviewed | Yes | en |
local.identifier.volume | 49 | en |
local.identifier.issue | 22 | en |
local.title.subtitle | Glycoconjugate Benzene Sulfonamides Prepared by "Click-Tailing" | en |
local.contributor.lastname | Wilkinson | en |
local.contributor.lastname | Bornaghi | en |
local.contributor.lastname | Houston | en |
local.contributor.lastname | Innocenti | en |
local.contributor.lastname | Supuran | en |
local.contributor.lastname | Poulsen | en |
dc.identifier.staff | une-id:bwilkin7 | en |
local.profile.orcid | 0000-0003-1866-6540 | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.identifier.unepublicationid | une:23094 | en |
local.identifier.handle | https://hdl.handle.net/1959.11/22910 | en |
dc.identifier.academiclevel | Academic | en |
local.title.maintitle | A Novel Class of Carbonic Anhydrase Inhibitors | en |
local.output.categorydescription | C1 Refereed Article in a Scholarly Journal | en |
local.search.author | Wilkinson, Brendan | en |
local.search.author | Bornaghi, Laurent F | en |
local.search.author | Houston, Todd A | en |
local.search.author | Innocenti, Alessio | en |
local.search.author | Supuran, Claudiu T | en |
local.search.author | Poulsen, Sally-Ann | en |
local.uneassociation | Unknown | en |
local.year.published | 2006 | en |
local.subject.for2020 | 340504 Organic green chemistry | en |
local.subject.for2020 | 340401 Biologically active molecules | en |
local.subject.for2020 | 340499 Medicinal and biomolecular chemistry not elsewhere classified | en |
local.subject.seo2020 | 280105 Expanding knowledge in the chemical sciences | en |
local.subject.seo2020 | 200199 Clinical health not elsewhere classified | en |
local.subject.seo2020 | 280102 Expanding knowledge in the biological sciences | en |
local.codeupdate.date | 2022-02-13T17:06:30.819 | en |
local.codeupdate.eperson | bwilkin7@une.edu.au | en |
local.codeupdate.finalised | true | en |
Appears in Collections: | Journal Article School of Science and Technology |
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