Synthesis, characterization, cytotoxicity, and DNA binding of some new platinum(II) and platinum(IV) complexes with benzimidazole ligands

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UTKU S., Gumus F., TEZCAN ÜLGER S., SERİN M. S., ÖZKUL A.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.25, no.4, pp.502-508, 2010 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 25 Issue: 4
  • Publication Date: 2010
  • Doi Number: 10.3109/14756360903282858
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.502-508
  • Keywords: Benzimidazole, cytotoxic activity, DNA binding, gel electrophoresis, platinum complexes, ANTITUMOR-ACTIVITY, RESISTANCE, ACID, MECHANISMS, REDUCTION, SPECTRA, MCF-7
  • Gazi University Affiliated: Yes

Abstract

In this study, two Pt(II) and three Pt(IV) complexes with the structures of [PtL2 Cl-2] (1), [PtL2 I-2] (2), [PtL2 Cl-2 (OH)(2)] (3), [PtL2Cl2 (OCOCH3)(2)] (4), and [PtL2Cl4] (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.