Synthesis, cytotoxic activity on MCF-7 cell line and mutagenic activity of platinum(II) complexes with 2-substituted benzimidazole ligands

Gumus F., Algul O., EREN G., Eorglu H., Diril N., Gur S., ...More

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol.38, no.5, pp.473-480, 2003 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 38 Issue: 5
  • Publication Date: 2003
  • Doi Number: 10.1016/s00223-5234(03)00058-8
  • Journal Name: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.473-480
  • Keywords: benzimidazole, Pt(II) complex, cytotoxic activity, mutagenic activity, ANTITUMOR COMPLEXES, CARRIER MOLECULES, IMIDAZOLE DONORS, AMINO-ACIDS, DNA-BINDING, CISPLATIN, RECOGNITION, THIAZOLE, PD(II), PT(II)
  • Gazi University Affiliated: Yes

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. (C) 2003 Editions scientifiques et medicales Elsevier SAS. All rights reserved.