Substituted 2,5'-bi-1H-benzimidazoles: Topoisomerase I inhibition and cytotoxicity

被引:264
作者
Kim, JS
Gatto, B
Yu, C
Liu, A
Liu, LF
LaVoie, EJ
机构
[1] RUTGERS STATE UNIV,DEPT PHARMACEUT CHEM,PISCATAWAY,NJ 08855
[2] UNIV MED & DENT NEW JERSEY,ROBERT WOOD JOHNSON MED SCH,DEPT PHARMACOL,PISCATAWAY,NJ 08855
关键词
D O I
10.1021/jm950412w
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several 2'-aryl-5-substituted-2,5'-bi-1H-benzimidazole derivatives were synthesized and evaluated as topoisomerase I poisons and for their cytotoxicity toward the human lymphoblast cell line RPMI 8402. This study focused on 18 2,5'-bi-1H-benzimidazole derivatives which contained either a 5-cyano, a 5-(aminocarbonyl), or a 5-(4-methylpiperazinyl) group. Among these bibenximidazoles, the pharmacological activity of 2'-phenyl derivatives and the influence of the different positional isomers of either a 2'-tolyl group or a 2'-naphthyl moiety on cytotoxicity and topoisomerase I inhibitory activity were determined.
引用
收藏
页码:992 / 998
页数:7
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