Synthesis, Cytotoxicity, and DNA Interactions of New Cisplatin Analogues Containing Substituted Benzimidazole Ligands

Basit Öğe Kaydı
dc.contributor.authorGümüş, Fatma
dc.contributor.authorEren, Gökçen
dc.contributor.authorAçık, Leyla
dc.contributor.authorÇelebi, Ayten
dc.contributor.authorÖztürk, Fatma
dc.contributor.authorYılmaz, Şükran
dc.contributor.authorElerman, Yalcin
dc.date.accessioned2020-06-25T17:48:32Z
dc.date.available2020-06-25T17:48:32Z
dc.date.issued2009
dc.departmentKırıkkale Üniversitesi
dc.descriptionOzkul, Aykut/0000-0001-5008-9443; Eren, Gokcen/0000-0002-3420-607X;
dc.description.abstractSix new platinum(II) complexes with 1-H or methyl-2-chloromethyl or acetoxymethyl or 2'-hydroxyethylbenzimidazole carrier ligands were synthesized and evaluated for their reactivity against model nucleophile I-, cellular uptake, and in vitro anti proliferative activities against the human MCF-7 breast and HeLa cervix cancer cell lines. The effect of the compounds on pBR322 plasmid DNA was studied by gel electrophoretic mobility measurements. Flow cytometric analysis was also carried out to study the effect of representative compounds 1 and 2, bearing 2-chloromethyl or -acetoxymethylbenzimidazole carrier ligands, on the cell cycle distribution of MCF-7 and HeLa cells, respectively. In general, it was found that Pt(II) complexes were less cytotoxic than cisplatin and were comparable to carboplatin. The results of the plasmid DNA interaction and the restriction studies suggest that changing the chemical structure of the benzimidazole ligands may modulate DNA binding mode and the sequence selectivity. Compounds I and 2 had no significant effect on the cell cycle profile of the cells used. However, Compound 2 induced a significant increase in the SubG1 cell population at a concentration of 20 mu M.en_US
dc.description.sponsorshipResearch Foundation of Gazi UniversityGazi University [EF-02/2002-06, EF-02/2004-28, 02/2007-24]en_US
dc.description.sponsorshipWe are grateful to Prof. Dr. Ibrahim Burgu (Faculty of Veterinary Medicine, Ankara University), Prof. Dr. Ali Sengul (Department of Immunology, Gulhane Military Medical Academia, Ankara) and Dr. Recep Ergal (Foot and Mouth Disease Institute, Ankara, Turkey) for their valuable support. For helpful assistance we thank Research Assistant Humay Akin (Faculty of Veterinary Medicine, Ankara University). We thank the Research Foundation of Gazi University (EF-02/2002-06, EF-02/2004-28 and 02/2007-24) for financial support.en_US
dc.identifier.citationclosedAccessen_US
dc.identifier.doi10.1021/jm8000983
dc.identifier.endpage1357en_US
dc.identifier.issn0022-2623
dc.identifier.issn1520-4804
dc.identifier.issue5en_US
dc.identifier.pmid19220055
dc.identifier.scopus2-s2.0-64349094401
dc.identifier.scopusqualityQ1
dc.identifier.startpage1345en_US
dc.identifier.urihttps://doi.org/10.1021/jm8000983
dc.identifier.urihttps://hdl.handle.net/20.500.12587/4487
dc.identifier.volume52en_US
dc.identifier.wosWOS:000263974700015
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherAmer Chemical Socen_US
dc.relation.ispartofJournal Of Medicinal Chemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.titleSynthesis, Cytotoxicity, and DNA Interactions of New Cisplatin Analogues Containing Substituted Benzimidazole Ligandsen_US
dc.typeArticle

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