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

dc.contributor.author Kuçükdumlu, Aslıgül
dc.contributor.author Güven, Ebru Bilget
dc.contributor.author Tunçbilek, Meral
dc.contributor.author Bilget Güven, Ebru
dc.contributor.author Atalay, Rengül Çetin
dc.contributor.other Molecular Biology and Genetics
dc.date.accessioned 2020-06-08T19:16:10Z
dc.date.available 2020-06-08T19:16:10Z
dc.date.issued 2020
dc.department Fakülteler, Mühendislik ve Doğa Bilimleri Fakültesi, Biyoinformatik ve Genetik Bölümü en_US
dc.description.abstract A 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.citationcount 3
dc.identifier.doi 10.17344/acsi.2019.5196 en_US
dc.identifier.endpage 82 en_US
dc.identifier.issn 1318-0207 en_US
dc.identifier.issn 1580-3155 en_US
dc.identifier.issn 1318-0207
dc.identifier.issn 1580-3155
dc.identifier.issue 1 en_US
dc.identifier.pmid 33558921 en_US
dc.identifier.scopus 2-s2.0-85082322472 en_US
dc.identifier.scopusquality Q3
dc.identifier.startpage 70 en_US
dc.identifier.uri https://hdl.handle.net/20.500.12469/2892
dc.identifier.uri https://doi.org/10.17344/acsi.2019.5196
dc.identifier.volume 67 en_US
dc.identifier.wos WOS:000521727500007 en_US
dc.institutionauthor Bilget Güven, Ebru en_US
dc.language.iso en en_US
dc.publisher Slovensko Kemijsko Drustvo en_US
dc.relation.journal Acta Chimica Slovenica en_US
dc.relation.publicationcategory Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı en_US
dc.rights info:eu-repo/semantics/openAccess en_US
dc.scopus.citedbyCount 5
dc.subject Purine en_US
dc.subject Piperazine en_US
dc.subject Benzyl en_US
dc.subject Cytotoxic activity en_US
dc.title Design, Synthesis and in Vitro Cytotoxic Activity of New 6,9-Disubstituted Purine Analogues en_US
dc.type Article en_US
dc.wos.citedbyCount 5
dspace.entity.type Publication
relation.isAuthorOfPublication 29a3046a-0e10-42f4-a54b-6ff546565470
relation.isAuthorOfPublication.latestForDiscovery 29a3046a-0e10-42f4-a54b-6ff546565470
relation.isOrgUnitOfPublication 71ce8622-7449-4a6a-8fad-44d881416546
relation.isOrgUnitOfPublication.latestForDiscovery 71ce8622-7449-4a6a-8fad-44d881416546

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