Design, Synthesis and In Vitro Cytotoxic Activity of New 6,9-Disubstituted Purine Analogues

dc.contributor.authorKuçükdumlu, Aslıgül
dc.contributor.authorTunçbilek, Meral
dc.contributor.authorBilget Güven, Ebru
dc.contributor.authorAtalay, Rengül Çetin
dc.date.accessioned2020-06-08T19:16:10Z
dc.date.available2020-06-08T19:16:10Z
dc.date.issued2020
dc.departmentFakülteler, Mühendislik ve Doğa Bilimleri Fakültesi, Biyoinformatik ve Genetik Bölümüen_US
dc.description.abstractA series of new 6,9-disubstituted purine analogs with 4-substituted piperazine at C-6 and 4-substituted benzyl at N-9 were designed and synthesized in four steps. All synthesized compounds (7-26) were screened initially for their in vitro anticancer activity on Huh7 liver, HCT116 colon and MCF7 breast carcinoma cell lines. Cytotoxic bioactivity studies revealed that all compounds screened, with compound 19 being the exception, were found to have promising cytotoxic activities at IC50 range of 0.05-21.8 mu M against cancer cells Huh7, HCT116 and MCF7. Among the prepared purine analogs, two of them (12 and 22) exhibited excellent cytotoxic activities, with IC50 0.08-0.13 mu M, on Huh7 cells comparable to camptothecin (CPT) and better than cladribine, fludarabine and 5-FU. Afterwards, the evaluation of cytotoxicity of the most potent purine analogs was screened against further hepatocellular cancer (HCC) cell lines. The 6-(4-(4-trifluoromethylphenyl)piperazine (12) and 6-(4-(3,4-dichlorophenyl)piperazine analogs (25) displayed a significant IC50 values (IC50 < 0.1-0.13 mu M) comparable to CPT and better cytotoxic bioactivity when compared with 5-FU, cladribine and fludarabine on HCC cells (Huh7 and HepG2).en_US
dc.identifier.citation3
dc.identifier.doi10.17344/acsi.2019.5196en_US
dc.identifier.endpage82en_US
dc.identifier.issn1318-0207en_US
dc.identifier.issn1580-3155en_US
dc.identifier.issn1318-0207
dc.identifier.issn1580-3155
dc.identifier.issue1en_US
dc.identifier.pmid33558921en_US
dc.identifier.scopus2-s2.0-85082322472en_US
dc.identifier.scopusqualityQ3
dc.identifier.startpage70en_US
dc.identifier.urihttps://hdl.handle.net/20.500.12469/2892
dc.identifier.urihttps://doi.org/10.17344/acsi.2019.5196
dc.identifier.volume67en_US
dc.identifier.wosWOS:000521727500007en_US
dc.identifier.wosqualityN/A
dc.institutionauthorBilget Güven, Ebruen_US
dc.language.isoenen_US
dc.publisherSlovensko Kemijsko Drustvoen_US
dc.relation.journalActa Chimica Slovenicaen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectPurineen_US
dc.subjectPiperazineen_US
dc.subjectBenzylen_US
dc.subjectCytotoxic activityen_US
dc.titleDesign, Synthesis and In Vitro Cytotoxic Activity of New 6,9-Disubstituted Purine Analoguesen_US
dc.typeArticleen_US
dspace.entity.typePublication

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