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Synthesis of 1,4-Bis(indolin Derivatives and Their Structure-Activity Relationships for the Interaction of Human Carbonic Anhydrase Isoforms I and II

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dc.authorscopusid8576446300
dc.authorscopusid6504284918
dc.authorscopusid22955598300
dc.authorscopusid37560999900
dc.authorscopusid23027537500
dc.contributor.authorTalaz, O.
dc.contributor.authorÇavdar, H.
dc.contributor.authorDurdagi, S.
dc.contributor.authorAzak, H.
dc.contributor.authorEkinci, D.
dc.date.accessioned2020-06-21T14:06:12Z
dc.date.available2020-06-21T14:06:12Z
dc.date.issued2013
dc.departmentOndokuz Mayıs Üniversitesien_US
dc.department-temp[Talaz] Oktay, Department of Chemistry, Karamanoğlu Mehmetbey Üniversitesi, Karaman, Karaman, Turkey; [Çavdar] Hüseyin, Education Faculty, Dumlupinar Üniversitesi, Kutahya, Turkey; [Durdagi] Serdar, Department of Biological Sciences, University of Calgary, Calgary, AB, Canada; [Azak] Hacer, Department of Chemistry, Karamanoğlu Mehmetbey Üniversitesi, Karaman, Karaman, Turkey; [Ekinci] Deniz, Department of Agricultural Biotechnology, Ondokuz Mayis Üniversitesi, Samsun, Turkeyen_US
dc.description.abstractSeveral 1,4-bis(indolin-1-ylmethyl)benzene-based compounds containing substituents such as five, six and seven cyclic derivatives on indeno part (9a-c) were prepared and tested against two members of the pH regulatory enzyme family, carbonic anhydrase (CA). The inhibitory potencies of the compounds at the human isoforms hCA I and hCA II targets were analyzed and K<inf>I</inf> values were calculated. K<inf>I</inf> values of compounds for hCA I and hCA II human isozymes were measured in the range of 39.3-42.6 μM and 0.17-0.29 μM, respectively. The structurally related compound indole was also tested in order to understand the structure-activity relationship. Most of the compounds showed good CA inhibitory efficacy. In silico docking studies of these derivatives within hCA I and II were also carried out and results are supported the kinetic assays. © 2012 Elsevier Ltd. All rights reserved.en_US
dc.identifier.doi10.1016/j.bmc.2012.09.027
dc.identifier.endpage1482en_US
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.issue6en_US
dc.identifier.pmid23121721
dc.identifier.scopus2-s2.0-84874550533
dc.identifier.scopusqualityQ2
dc.identifier.startpage1477en_US
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2012.09.027
dc.identifier.volume21en_US
dc.identifier.wosWOS:000315573800015
dc.identifier.wosqualityQ1
dc.language.isoenen_US
dc.publisherPergamon-Elsevier Science Ltden_US
dc.relation.ispartofBioorganic & Medicinal Chemistryen_US
dc.relation.journalBioorganic & Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectBisindoleen_US
dc.subjectCarbonic Anhydraseen_US
dc.subjectDockingen_US
dc.subjectGlaucomaen_US
dc.titleSynthesis of 1,4-Bis(indolin Derivatives and Their Structure-Activity Relationships for the Interaction of Human Carbonic Anhydrase Isoforms I and IIen_US
dc.typeArticleen_US
dspace.entity.typePublication

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