SYNTHESIS AND EVALUATION OF TERBENZIMIDAZOLES AS TOPOISOMERASE-I INHIBITORS

被引：78

作者：

SUN, Q

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 38卷 / 18期

关键词：

D O I：

10.1021/jm00018a024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.

引用

页码：3638 / 3644

页数：7

共 35 条

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