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dc.contributor.authorSitaRam
dc.contributor.authorÇelik, Gülşah
dc.contributor.authorKhloya, Poonam
dc.contributor.authorVullo, Daniela
dc.contributor.authorSupuran, Claudiu T.
dc.contributor.authorSharma, Pawan K.
dc.date.accessioned2019-10-17T10:53:25Z
dc.date.available2019-10-17T10:53:25Z
dc.date.issued2014en_US
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2014.01.055
dc.identifier.urihttps://hdl.handle.net/20.500.12462/8297
dc.descriptionÇelik, Gülşah (Balıkesir Author)en_US
dc.description.abstractThree series of novel heterocyclic compounds (3a-3g, 4a-4g and 5a-5g) containing benzenesulfonamide moiety and incorporating a 1,2,4-triazole ring, have been synthesized and investigated as inhibitors against four isomers of the alpha-class carbonic anhydrases (CAs, EC 4.2.1.1), comprising hCAs I and II (cytosolic, ubiquitous isozymes) and hCAs IX and XII (transmembrane, tumor associated isozymes). Against the human isozymes hCA I and II, compounds of two series (3a-3g and 4a-4g) showed K-i values in the range of 84-868 nM and 5.6-390 nM, respectively whereas compounds of series 5a-5g were found to be poor inhibitors (K-i values exceeding 10,000 nM in some cases). Against hCA IX and XII, all the tested compounds exhibited excellent to moderate inhibitory potential with K-i values in the range of 2.8-431 nM and 1.3-63 nM, respectively. Compounds 3d, 3f and 4f exhibited excellent inhibitory potential against all of the four isozymes hCA I, II, IX and XII, even better than the standard drug acetazolamide (AZA) whereas compound of the series 5a-5g were comparatively less potent but more selective towards hCA IX and XII.en_US
dc.description.sponsorshipCouncil of Scientific and Industrial Research, New Delhi, India Haryana State Council for Science and Technology (HSCST), Panchkula (Haryana), India EUen_US
dc.language.isoengen_US
dc.publisherPergamon-Elsevier Science Ltden_US
dc.relation.isversionof10.1016/j.bmc.2014.01.055en_US
dc.rightsinfo:eu-repo/semantics/embargoedAccessen_US
dc.subjectTriazolesen_US
dc.subjectBenzenesulfonamideen_US
dc.subjectCarbonic Anhydrase İsoforms I, II, IX, XIIen_US
dc.subjectAcetazolamideen_US
dc.titleBenzenesulfonamide bearing 1,2,4-triazole scaffolds as potent inhibitors of tumor associated carbonic anhydrase isoforms hCA IX and hCA XIIen_US
dc.typearticleen_US
dc.relation.journalBioorganic & Medicinal Chemistryen_US
dc.contributor.departmentFen-Edebiyat Fakültesien_US
dc.contributor.authorID0000-0001-6613-1634en_US
dc.identifier.volume22en_US
dc.identifier.issue6en_US
dc.identifier.startpage1873en_US
dc.identifier.endpage1882en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US


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