Synthesis, characterization and in vitro cytotoxic, mutagenic and antimicrobial activity of platinum(II) complexes with substituted benzimidazole ligands

被引:67
作者
Gümüs, F
Pamuk, I
Özden, T
Yildiz, S
Diril, N
Öksüzoglu, E
Gür, S
Özkul, A
机构
[1] Gazi Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06330 Etiler Ankara, Turkey
[2] Ankara Univ, Fac Pharm, Dept Pharmaceut Microbiol, TR-06100 Ankara, Turkey
[3] Hacettepe Univ, Fac Sci, Dept Mol Biol, TR-06532 Ankara, Turkey
[4] Afyon Kocatepe Univ, Fac Vet Med, Dept Microbiol, Afyon, Turkey
[5] Ankara Univ, Fac Vet Med, Dept Virol, TR-06100 Ankara, Turkey
关键词
benzimidazole; Pt(II) complexes; Pt(II) complex cytotoxic activity; Pt(II) complex mutagenic activity;
D O I
10.1016/S0162-0134(03)00005-9
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In this study, six Pt(II) complexes bearing 5(6)-H or -CH3-2-phenyl or -(2'-pyridyl) or -mercaptomethylbenzimidazole ligands as,carrier groups' were synthesized and characterized by elemental analysis, IR and H-1-NMR spectra and evaluated for their preliminary in vitro cytotoxic activity to the human RD Rhabdomyosarcoma cell line and mutagenic properties in Salmonella typhimurium strains TA 98 and TA 100 in the absence of the S9 rat liver fraction. The preliminary test results showed that the complexes had slightly greater cytotoxic activity on the RD cell line at 1 muM concentration than cisplatin. Among the compounds tested for their mutagenicity, Pt(II) complexes of 2-(2'-pyridyl)- and 5(6)-methyl-2-(2'-pyridyl)benzimidazoles were found to be mutagenic. A comparative study of the MIC (minimum inhibitory concentration) values indicated that, in general, there were no differences between the poor antimicrobial activity values of the ligands and their Pt(II) complexes with respect to the tested microorganisms. These results suggest that the synthesized Pt(II) complexes should be considered for further antitumor activity studies. (C) 2003 Elsevier Science Inc. All rights reserved.
引用
收藏
页码:255 / 262
页数:8
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