Cytotoxic activity of 4 '-hydroxychalcone derivatives against Jurkat cells and their effects on mammalian DNA topoisomerase I

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dc.contributor.authorGul, Halise Inci
dc.contributor.authorCizmecioglu, Murat
dc.contributor.authorZencir, Sevil
dc.contributor.authorGul, Mustafa
dc.contributor.authorCanturk, Pakize
dc.contributor.authorAtalay, Mustafa
dc.contributor.authorTopcu, Zeki
dc.date.accessioned2019-10-27T20:21:01Z
dc.date.available2019-10-27T20:21:01Z
dc.date.issued2009
dc.departmentEge Üniversitesien_US
dc.description.abstractChalcones (1,3-diaryl-2-propen-1-ones) are alpha, beta-unsaturated ketones with cytotoxic and anticancer properties. Several reports have shown that compounds with cytotoxic properties may also interfere with DNA topoisomerase functions. Five derivatives of 4'-hydroxychalcones were examined for cytotoxicity against transformed human T (Jurkat) cells as well as plasmid supercoil relaxation experiments using mammalian DNA topoisomerase I. The compounds were 3-phenyl-1-(4'-hydroxyphenyl)-2-propen-1-one (I), 3-(p-methylphenyl)-1-(4'-hydroxyphenyl)-2-propen-1-one (II), 3-(p-methoxyphenyl)-1-(4'-hydroxyphenyl)-2-propen-1-one (III), 3-(p-chlorophenyl)-1-(4'-hydroxyphenyl)-2-propen-1-one (IV), and 3-(2- thienyl)-1-(4'-hydroxyphenyl)-2-propen-1-one (V). The order of the cytotoxicity of the compounds was; IV > III > II > I > V. Compound IV, had the highest Hammett and log P values (0.23 and 4.21, respectively) and exerted both highest cytotoxicity and strongest DNA topoisomerase I inhibition. Compounds I and II gave moderate interference with the DNA topoisomerase I while III & V did not interfere with the enzyme.en_US
dc.identifier.doi10.1080/14756360802399126en_US
dc.identifier.endpage807en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue3en_US
dc.identifier.pmid18830876en_US
dc.identifier.startpage804en_US
dc.identifier.urihttps://doi.org/10.1080/14756360802399126
dc.identifier.urihttps://hdl.handle.net/11454/41708
dc.identifier.volume24en_US
dc.identifier.wosWOS:000266040700025en_US
dc.identifier.wosqualityQ3en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_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.subject4 '-hydroxychalconeen_US
dc.subjectcytotoxicityen_US
dc.subjectJurkat cellsen_US
dc.subjectMTTen_US
dc.subjectDNA topoisomerase Ien_US
dc.subjectinhibitionen_US
dc.titleCytotoxic activity of 4 '-hydroxychalcone derivatives against Jurkat cells and their effects on mammalian DNA topoisomerase Ien_US
dc.typeArticleen_US

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