Biological activity of bis-benzimidazole derivatives on DNA topoisomerase i and HeLa, MCF7 and A431 cells

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dc.contributor.authorAlpan A.S.
dc.contributor.authorZencir S.
dc.contributor.authorZupkó I.
dc.contributor.authorCoban G.
dc.contributor.authorRthy B.
dc.contributor.authorGunes H.S.
dc.contributor.authorTopcu Z.
dc.date.accessioned2019-10-27T08:36:17Z
dc.date.available2019-10-27T08:36:17Z
dc.date.issued2009
dc.departmentEge Üniversitesien_US
dc.description.abstractBenzimidazoles of both natural and synthetic sources are the key components of many bio-active compounds. Several reports have shown antifungal, antiviral, H2 receptor blocker and antitumor activities for benzimidazoles and their derivatives. In this study, we synthesized twelve bis-benzimidazole derivatives by selecting di(1H-benzo[d]imidazol-2-yl)methane as the main compound. The numbers of carbons at 2 positions of bis-benzimidazole derivatives were changed from 1 to 4, and derivatives were synthesized with methyl substitutions at 5- and/or 6- positions. The compounds were screened via in vitro plasmid superciol relaxation assays using mammalian DNA topoisomerase I and cytostatic assays were carried out against HeLa (cervix adenocarcinoma), MCF7 (breast adenocarcinoma) and A431 (skin epidermoid carcinoma) cells for selected derivatives. Our results suggest that the malonic acid derivatives of bis-benzimidazoles, namely, bis(5-methyl-1H-benzo[d]imidazol-2-yl)methane and bis(5,6-dimethyl-1H-benzo[d] imidazol-2-yl)methane, were remarkably active compounds in interfering with DNA topoisomerase I and the former compound was also found to be cytotoxic against MCF7 and A431 cells. The inhibitory effects obtained with these derivatives are significant as these compounds can be potential sources of anticancer agents. © 2009 Informa UK Ltd.en_US
dc.identifier.doi10.1080/14756360802420831en_US
dc.identifier.endpage849en_US
dc.identifier.issn1475-6366
dc.identifier.issue3en_US
dc.identifier.pmid18951286en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage844en_US
dc.identifier.urihttps://doi.org/10.1080/14756360802420831
dc.identifier.urihttps://hdl.handle.net/11454/27368
dc.identifier.volume24en_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherInforma Healthcareen_US
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectBis-benzimidazolesen_US
dc.subjectCytotostaticityen_US
dc.subjectDNA topoisomerase Ien_US
dc.titleBiological activity of bis-benzimidazole derivatives on DNA topoisomerase i and HeLa, MCF7 and A431 cellsen_US
dc.typeArticleen_US

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