Design, synthesis and biological evaluation of novel nitroaromatic compounds as potent glutathione reductase inhibitors

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dc.contributor.authorCakmak, Resit
dc.contributor.authorDurdagi, Serdar
dc.contributor.authorEkinci, Deniz
dc.contributor.authorSenturk, Murat
dc.contributor.authorTopal, Giray
dc.date.accessioned2024-04-24T16:10:57Z
dc.date.available2024-04-24T16:10:57Z
dc.date.issued2011
dc.departmentDicle Üniversitesien_US
dc.description.abstractDiscovery of GR inhibitors has become very popular recently due to antimalarial and anticancer activities. In this study, the synthesis and GR inhibitory capacities of novel nitroaromatic compounds (NCs) (1-3) were reported. Some commercially available molecules were also tested for comparison reasons. The novel NCs were obtained in high yields using simple chemical procedures and exhibited much potent inhibitory activities against GR at low micromolar concentrations with K-i values ranging from 0.211 to 4.57 mu M as compared with well-known agents. Inhibition mechanism was assessed as being due to occlusion of the active site entrance by means of the NCs. Molecular docking results have shown that docking poses of ligands are able to construct binding interactions with the essential amino acids. (C) 2011 Elsevier Ltd. All rights reserved.en_US
dc.description.sponsorshipScientific and Technical Research Council of Turkey (TUBITAK) [110T507]en_US
dc.description.sponsorshipThe authors greatly acknowledge the Scientific and Technical Research Council of Turkey (TUBITAK) for financial support (Project No: 110T507) for (G.T. and R.C.).en_US
dc.identifier.doi10.1016/j.bmcl.2011.07.002
dc.identifier.endpage5402en_US
dc.identifier.issn0960-894X
dc.identifier.issn1464-3405
dc.identifier.issue18en_US
dc.identifier.pmid21795044
dc.identifier.scopus2-s2.0-80051932732
dc.identifier.scopusqualityQ2
dc.identifier.startpage5398en_US
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2011.07.002
dc.identifier.urihttps://hdl.handle.net/11468/15198
dc.identifier.volume21en_US
dc.identifier.wosWOS:000294051800056
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoenen_US
dc.publisherPergamon-Elsevier Science Ltden_US
dc.relation.ispartofBioorganic & Medicinal Chemistry Letters
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectGlutathione Reductaseen_US
dc.subjectAntimalariaen_US
dc.subjectNitroaromaticen_US
dc.subjectIn Silico Dockingen_US
dc.titleDesign, synthesis and biological evaluation of novel nitroaromatic compounds as potent glutathione reductase inhibitorsen_US
dc.titleDesign, synthesis and biological evaluation of novel nitroaromatic compounds as potent glutathione reductase inhibitors
dc.typeArticleen_US

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