9,10-Dibromo-N-aryl-9,10-dihydro-9,10-[3,4]epipyrroloanthracene-12,14-diones: Synthesis and Investigation of Their Effects on Carbonic Anhydrase Isozymes I, II, IX, and XII

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dc.contributor.authorGöksu, Haydar
dc.contributor.authorTopal, Meryem
dc.contributor.authorKeskin, Ali
dc.contributor.authorGültekin, Mehmet S.
dc.contributor.authorÇelik, Murat
dc.contributor.authorGülçin, İlhami
dc.contributor.authorSupuran, Claudiu T.
dc.date.accessioned2020-04-30T22:38:35Z
dc.date.available2020-04-30T22:38:35Z
dc.date.issued2016
dc.departmentDÜ, Kaynaşlı Meslek Yüksekokuluen_US
dc.descriptionGULCIN, Ilhami/0000-0001-5993-1668en_US
dc.descriptionWOS: 000380022500007en_US
dc.descriptionPubMed: 27174792en_US
dc.description.abstractN-substituted maleimides were synthesized from maleic anhydride and primary amines. 1,4-Dibromodibenzo[e,h]bicyclo-[2,2,2]octane-2,3-dicarboximide derivatives (4a-f) were prepared by the [4+2] cycloaddition reaction of dibromoanthracenes with the N-substituted maleimide derivatives. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the new derivatives were assayed against the human (h) isozymes hCA I, II, IX, and XII. All tested bicyclo dicarboximide derivatives exhibited excellent inhibitory effects in the nanomolar range, with K-i values in the range of 117.73-232.87 nM against hCA I and of 69.74-111.51 nM against hCA II, whereas they were low micromolar inhibitors against hCA IX and XII.en_US
dc.description.sponsorshipDepartments of Chemistry at Ataturk UniversityAtaturk University; TUBA (Turkish Academy of Sciences)Turkish Academy of Sciences; Research Chairs Program at King Saud University; EUEuropean Union (EU)en_US
dc.description.sponsorshipThe authors are indebted to Departments of Chemistry at Ataturk University and TUBA (Turkish Academy of Sciences) for their support of this work. I.G. would like to extend his sincere appreciation to the Research Chairs Program at King Saud University for funding this research. Work from the Florence lab was financed by a EU FP7 project (Dynano).en_US
dc.identifier.doi10.1002/ardp.201600047en_US
dc.identifier.endpage474en_US
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue6en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage466en_US
dc.identifier.urihttps://doi.org/10.1002/ardp.201600047
dc.identifier.urihttps://hdl.handle.net/20.500.12684/2275
dc.identifier.volume349en_US
dc.identifier.wosWOS:000380022500007en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakPubMeden_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofArchiv Der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectEnzyme inhibitionen_US
dc.subjectEnzyme purificationen_US
dc.subjectIsoenzymeen_US
dc.title9,10-Dibromo-N-aryl-9,10-dihydro-9,10-[3,4]epipyrroloanthracene-12,14-diones: Synthesis and Investigation of Their Effects on Carbonic Anhydrase Isozymes I, II, IX, and XIIen_US
dc.typeArticleen_US

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