Synthesis, characterization, cytotoxicity, and DNA binding of some new platinum(II) and platinum(IV) complexes with benzimidazole ligands.
In this study, two Pt(II) and three Pt(IV) complexes with the structures of [PtL(2)Cl(2)] (1), [PtL(2)I(2)] (2), [PtL(2)Cl(2)(OH)(2)] (3), [PtL(2)Cl(2)(OCOCH(3))(2)] (4), and [PtL(2)Cl(4)] (5) (L = benzimidazole as carrier ligand) were synthesized and evaluated for their in vitro antiproliferative activities against the human MCF-7, HeLa, and HEp-2 cancer cell lines. The influence of compounds 1-5 on the tertiary structure of DNA was determined by their ability to modify the electrophoretic mobility of the form I and II bands of pBR322 plasmid DNA. The inhibition of BamH1 restriction enzyme activity of compounds 1-5 was also determined. In general, it was found that compounds 1-5 were less active than cisplatin and carboplatin against MCF-7 and HeLa cell lines (except for 1, which was found to be more active than carboplatin against the MCF-7 cell line). Compounds 1 and 3 were found to be significantly more active than cisplatin and carboplatin against the HEp-2 cell line.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Mersin, Mersin, Turkey.
Semra
S
Utku
Fatma
F
Gumus
Seda
S
Tezcan
Mehmet Sami
MS
Serin
Aykut
A
Ozkul
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001562:Benzimidazoles / Q000737:chemistry*; D016190:Carboplatin / Q000494:pharmacology; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000494:pharmacology; D004247:DNA / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D009690:Nucleic Acid Conformation / Q000187:drug effects; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D010957:Plasmids; D010984:Platinum
D000970:Antineoplastic Agents; D001562:Benzimidazoles; D008024:Ligands; D009942:Organometallic Compounds; D010984:Platinum; D004247:DNA; D016190:Carboplatin; C031000:benzimidazole; D002945:Cisplatin