A SAR Study: Evaluation of Bromo Derivatives of 8-Substituted Quinolines as Novel Anticancer Agents

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dc.contributor.authorOkten, Salih
dc.contributor.authorCakmak, Osman
dc.contributor.authorTekin, Saban
dc.contributor.authorKoprulu, Tugba Kul
dc.date.accessioned2020-06-25T18:23:29Z
dc.date.available2020-06-25T18:23:29Z
dc.date.issued2017
dc.departmentKırıkkale Üniversitesi
dc.descriptionOkten, Salih/0000-0001-9656-1803
dc.description.abstractBackground: Brominated 8-hydroxy, 8-methoxy, 8-amino quinolines 5, 6, 8, 9 and novel cyano 8-hydroxyquinolines 11, 12 were evaluated in vitro for their anticancer effects on various cell lines. 5,7-Dibromo-5, 7-bromo-6, 7-cyano-11 and 5,7-dicyano-12 8-hydroxyquinolines were shown to have strong antiproliferative activity against various tumor cell lines, including C6 (rat brain tumor), HeLa (human cervix carcinoma), and HT29 (human colon carcinoma) with IC50 values ranged from 6.7 to 25.6 mu g/mL. Methods: A structure activity relationship (SAR) was conducted that quinoline core containing hydroxly group at C-8 positon led to more anti cancer potentials. Results: The results of Lactate Dehydrogenase (LDH) cytotoxic, DNA laddering and inhibition assays indicated that 5, 6, 11 and 12 have high cytotoxic effects and appototic potentials. Conclusion: Furthermore, 5 and 12 have inhibitory effects on relaxation of supercoiled plazmid DNA by supressed the Topoisomerase I enzyme. As a result, 5, 6, 11 and 12 may have promising anticancer drug potential and 5 and 12 may be novel topoisomerase inhibitors.en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [112T394]; Kirikkale University Research FundKirikkale University [2012/122]en_US
dc.description.sponsorshipThis study was financially supported by grants from the Scientific and Technological Research Council of Turkey (TUBITAK, Project number: 112T394) and Kirikkale University Research Fund (Project number: 2012/122).en_US
dc.identifier.citationclosedAccessen_US
dc.identifier.doi10.2174/1570180814666170504150050
dc.identifier.endpage1424en_US
dc.identifier.issn1570-1808
dc.identifier.issn1875-628X
dc.identifier.issue12en_US
dc.identifier.scopus2-s2.0-85038858819
dc.identifier.scopusqualityQ3
dc.identifier.startpage1415en_US
dc.identifier.urihttps://doi.org/10.2174/1570180814666170504150050
dc.identifier.urihttps://hdl.handle.net/20.500.12587/7114
dc.identifier.volume14en_US
dc.identifier.wosWOS:000414248000009
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherBentham Science Publ Ltden_US
dc.relation.ispartofLetters In Drug Design & Discovery
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectSARen_US
dc.subjectbrominationen_US
dc.subjecthydroxyquinolineen_US
dc.subjectmethoxyquinolineen_US
dc.subjectcyanoquinolineen_US
dc.subjectanticancer effecten_US
dc.subjectcytotoxicityen_US
dc.subjectantitopoisomeraseen_US
dc.titleA SAR Study: Evaluation of Bromo Derivatives of 8-Substituted Quinolines as Novel Anticancer Agentsen_US
dc.typeArticle

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