1H-benzimidazole derivatives as mammalian DNA topoisomerase I inhibitors

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dc.contributor.authorAlpan, A. Selcen
dc.contributor.authorGunesi, H. Sernih
dc.contributor.authorTopcu, Zeki
dc.date.accessioned2019-10-27T19:36:54Z
dc.date.available2019-10-27T19:36:54Z
dc.date.issued2007
dc.departmentEge Üniversitesien_US
dc.description.abstractBenzimidazole is one of the most important heterocyclic groups manifesting various biological properties, such as antibacterial, antifungal, antimicrobial, antiprotozoal and antihelmintic activities. Several benzimidazole derivatives are also active as inhibitors of type I DNA topoisomerases. In this study, three 1H-benzimidazole derivatives with different electronic characteristics at position 5-, namely 5-chloro-4-(1H-benzimidazole-2-yl)phenoI (Cpd I), 5-methyl-4-(1H-benzimidazole-2-yl)phenol (Cpd II) and 4-(1H-benzimidazole-2-yl)phenol (Cpd III), were synthesized and evaluated for their effects on mammalian type I DNA topoisomerase activity using quantitative in vitro plasmid supercoil relaxation assays. For the structure elucidation of the compounds, melting points, UV, IR, H-1 NMR, C-13 NMR, mass spectral data and elemental analyses were interpreted. Among the compounds, 5-methyl-4-(1H-benzimidazole-2-yl)phenoI (Cpd II) manifested relatively potent topoisomerase I inhibition.en_US
dc.identifier.endpage565en_US
dc.identifier.issn0001-527X
dc.identifier.issue3en_US
dc.identifier.pmid17823665en_US
dc.identifier.scopusqualityN/Aen_US
dc.identifier.startpage561en_US
dc.identifier.urihttps://hdl.handle.net/11454/39911
dc.identifier.volume54en_US
dc.identifier.wosWOS:000249819500011en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherActa Biochimica Polonicaen_US
dc.relation.ispartofActa Biochimica Polonicaen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subject1H-benzimidazole derivativesen_US
dc.subjecttype I DNA topoisomeraseen_US
dc.subjectplasmid supercoil relaxation assaysen_US
dc.title1H-benzimidazole derivatives as mammalian DNA topoisomerase I inhibitorsen_US
dc.typeArticleen_US

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