title: Synthesis, cytotoxic activity on MCF-7 cell line and mutagenic activity of platinum(II) complexes with 2-substituted benzimidazole ligands.
abstract: Four Pt(II) complexes with 2-H/or-methyl/or-aminomethylbenzimidazole or 1,2-dimethylbenzimidazole ligands as "non-leaving groups" were synthesized and their antiproliferative properties were tested against the human MCF-7 breast cancer cell line. The mutagenic potentials of the complexes were tested in Salmonella typhimurium strains TA 98 and TA 100 in the absence of S9 rat liver fraction. In general, Pt(II) complexes tested which were found to be less active than cisplatin, exhibited moderate in vitro cytotoxic activity on MCF-7 cell line. Among the complexes tested, Pt(II) complex with 2-aminomethylbenzimidazole ligand was found to be highly mutagenic in S. typhimurium TA 98 and low mutagenic in S. typhimurium TA 100. Pt(II) complex with 1,2-dimethylbenzimidazole was mutagenic only in S. typhimurium TA 98. The other two complexes were found to be non-mutagen in both strains.
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Gazi, 06330 Etiler, Ankara, Turkey. gumusf@pharmacy.gazi.edu.tr
authors.forename: Fatma
authors.initials: F
authors.lastname: Gümüş
authors.forename: Oztekin
authors.initials: O
authors.lastname: Algül
authors.forename: Gökçen
authors.initials: G
authors.lastname: Eren
authors.forename: Hatice
authors.initials: H
authors.lastname: Eroğlu
authors.forename: Nuran
authors.initials: N
authors.lastname: Diril
authors.forename: Sibel
authors.initials: S
authors.lastname: Gür
authors.forename: Aykut
authors.initials: A
authors.lastname: Ozkul
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy; D002945:Cisplatin / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D009152:Mutagenicity Tests; D009153:Mutagens / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D012016:Reference Values; D012486:Salmonella typhimurium / Q000187:drug effects / Q000235:genetics; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D008024:Ligands; D009153:Mutagens; D009944:Organoplatinum Compounds; C031000:benzimidazole; D002945:Cisplatin