REVERSAL OF MULTIDRUG RESISTANCE IN HUMAN KB CELL-LINES BY STRUCTURAL ANALOGS OF VERAPAMIL

被引:60
作者
PIRKER, R
KEILHAUER, G
RASCHACK, M
LECHNER, C
LUDWIG, H
机构
[1] MED CLIN 2,A-1090 VIENNA,AUSTRIA
[2] KNOLL AG,W-6700 LUDWIGSHAFEN,GERMANY
关键词
D O I
10.1002/ijc.2910450523
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
Several structural analogs of verapamil were studied for their ability to reverse multi‐drug resistance (MDR) in human KB cell lines. D595, D792 and verapamil completely reversed resistance to colchicine and adriamycin. D595 and D792 had a higher reversing potency than verapamil. Devapamil, gallopamil, emopamil and D528 partially reversed MDR. The reversing potency of a drug did not correlate with its calcium antagonistic activity. No differences in reversing potency between (R)‐isomers, (L)‐isomers and the racemic forms were observed in the case of both verapamil and emopamil. (R)‐verapamil, which has less calcium antagonistic activity and less in vivo toxicity than racemic verapamil, and D792, which has higher reversing potency and less in vivo toxicity than racemic verapamil, should be suitable for clinical applications to overcome drug resistance in cancer patients. Copyright © 1990 Wiley‐Liss, Inc., A Wiley Company
引用
收藏
页码:916 / 919
页数:4
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