Synthesis of novel 6-substituted amino-9-(β-D-ribofuranosyl)purine analogs and their bioactivities on human epithelial cancer cells

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dc.citation.epage239en_US
dc.citation.issueNumber3en_US
dc.citation.spage235en_US
dc.citation.volumeNumber28en_US
dc.contributor.authorTuncbilek, M.en_US
dc.contributor.authorKucukdumlu, A.en_US
dc.contributor.authorGuven, E. B.en_US
dc.contributor.authorAltiparmak, D.en_US
dc.contributor.authorCetin Atalay, R.en_US
dc.date.accessioned2019-02-21T16:01:24Zen_US
dc.date.available2019-02-21T16:01:24Zen_US
dc.date.issued2018en_US
dc.departmentDepartment of Molecular Biology and Geneticsen_US
dc.description.abstractNew nucleoside derivatives with nitrogen substitution at the C-6 position were prepared and screened initially for their in vitro anticancer bioactivity against human epithelial cancer cells (liver Huh7, colon HCT116, breast MCF7) by the NCI-sulforhodamine B assay. N6-(4-trifluoromethylphenyl)piperazine analog (27) exhibited promising cytotoxic activity. The compound 27 was more cytotoxic (IC50 = 1-4 μM) than 5-FU, fludarabine on Huh7, HCT116 and MCF7 cell lines. The most potent nucleosides (11, 13, 16, 18, 19, 21, 27, 28) were further screened for their cytotoxicity in hepatocellular cancer cell lines. The compound 27 demonstrated the highest cytotoxic activity against Huh7, Mahlavu and FOCUS cells (IC50 = 1, 3 and 1 μM respectively). Physicochemical properties, drug-likeness, and drug score profiles of the molecules showed that they are estimated to be orally bioavailable. The results pointed that the novel derivatives would be potential drug candidates.en_US
dc.description.provenanceMade available in DSpace on 2019-02-21T16:01:24Z (GMT). No. of bitstreams: 1 Bilkent-research-paper.pdf: 222869 bytes, checksum: 842af2b9bd649e7f548593affdbafbb3 (MD5) Previous issue date: 2018en_US
dc.description.sponsorshipThis work was supported by the Scientific and Technological Research Council of Turkey -TUBITAK ( TBAG-109T987 ), the KANSIL-2016H121540 ( Ministry of Development , Turkey). Aen_US
dc.embargo.release2020-02-01en_US
dc.identifier.doi10.1016/j.bmcl.2017.12.070en_US
dc.identifier.eissn1464-3405en_US
dc.identifier.issn0960-894Xen_US
dc.identifier.urihttp://hdl.handle.net/11693/49841en_US
dc.language.isoEnglishen_US
dc.publisherElsevieren_US
dc.relation.isversionofhttps://doi.org/10.1016/j.bmcl.2017.12.070en_US
dc.relation.projectKANSIL-2016H121540 - TBAG-109T987en_US
dc.source.titleBioorganic and Medicinal Chemistry Lettersen_US
dc.subjectCytotoxic activityen_US
dc.subjectHepatocellular carcinomaen_US
dc.subjectMicrowave-assisted synthesisen_US
dc.subjectNucleoside analogsen_US
dc.titleSynthesis of novel 6-substituted amino-9-(β-D-ribofuranosyl)purine analogs and their bioactivities on human epithelial cancer cellsen_US
dc.typeArticleen_US

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