Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b] indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI

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dc.authorid0000-0003-2209-5402en_US
dc.contributor.authorEkinci, Deniz
dc.contributor.authorÇavdar, Hüseyin
dc.contributor.authorDurdağı, Serdar
dc.contributor.authorTalaz, Oktay
dc.contributor.authorŞentürk, Murat
dc.contributor.authorSupuran, Claudiu T.
dc.date.accessioned2019-12-06T21:02:14Z
dc.date.available2019-12-06T21:02:14Z
dc.date.issued2012
dc.departmentKMÜ, Kamil Özdağ Fen Fakültesi, Kimya Bölümüen_US
dc.descriptionWOS:000302033300006en_US
dc.descriptionPubMed:22245047en_US
dc.description.abstractSeveral 5,10-dihydroindeno[1,2-b]indole derivatives incorporating methoxy, hydroxyl, and halogen (F, Cl, and Br) moieties on the indene fragment of the molecule were prepared and tested against five carbonic anhydrase (CA, EC 4.2.1.1) isoforms. The inhibitory potencies of these compounds against the human (h) isoforms hCA I, II, IV, VI and bovine (b) isoform bCA III were assessed. Most of them exhibited low micromolar inhibition of these enzymes. K-I values of these compounds against hCA I and hCA II were in the range of 2.14-16.32 mu M, and 0.34-2.52 mu M, respectively. Isozyme hCA IV was inhibited with K-I-s in the range of 0.435-5.726 mu M, while hCA VI with K-I-s of 1.92-12.84 mu M bCA III was inhibited with K-I-s in the range of 2.13-17.83 mu M. The structurally related compounds, 1,2-dimethoxybenzene, catechol and indole were also tested in order to understand the structure activity relationship. In silico docking studies of some derivatives within the active site of hCA I and II were also carried out in order to rationalize the inhibitory properties of these compounds and understand their inhibition mechanism. (C) 2011 Elsevier Masson SAS. All rights reserved.en_US
dc.description.sponsorshipTurkish Republic Prime Ministry State Planning Organization (DPT)Turkiye Cumhuriyeti Kalkinma Bakanligi [2010K120440]; Agri Ibrahim Cecen University Scientific Research CouncilAgri Ibrahim Cecen University [Agri BAP-2010/K-10]; EUEuropean Union (EU)en_US
dc.description.sponsorshipThis study was financed by Turkish Republic Prime Ministry State Planning Organization (DPT), (Project no: 2010K120440) and Agri Ibrahim Cecen University Scientific Research Council, (Project no: Agri BAP-2010/K-10) for (MS) and by an FP7 EU grant to CTS (Metoxia).en_US
dc.identifier.citationEkinci, D., Çavdar, H., Durdağı, S., Talaz, O., Şentürk, M., Supuran, C. T. (2012). Structure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-<b>b</b>]indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VI. European Journal of Medicinal Chemistry, 49, 68-73.
dc.identifier.doi10.1016/j.ejmech.2011.12.022
dc.identifier.endpage73en_US
dc.identifier.issn0223-5234
dc.identifier.issn1768-3254
dc.identifier.pmid22245047
dc.identifier.startpage68en_US
dc.identifier.urihttps://dx.doi.org/10.1016/j.ejmech.2011.12.022
dc.identifier.urihttps://hdl.handle.net/11492/2219
dc.identifier.volume49en_US
dc.identifier.wosWOS:000302033300006
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Sceince
dc.indekslendigikaynakPubMed
dc.institutionauthorTalaz, Oktay
dc.language.isoen
dc.publisherElsevier France - Editions Scientifiques Medicales Elsevieren_US
dc.relation.journalEuropean Journal of Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectCarbonic Anhydraseen_US
dc.subjectPhenol Inhibitoren_US
dc.subjectSulfonamide Inhibitoren_US
dc.subjectDockingen_US
dc.subjectIndoleen_US
dc.titleStructure-activity relationships for the interaction of 5,10-dihydroindeno[1,2-b] indole derivatives with human and bovine carbonic anhydrase isoforms I, II, III, IV and VIen_US
dc.typeArticle

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