CONFORMATIONS, DNA BINDING PARAMETERS, AND ANTI-LEUKEMIC ACTIVITY OF CERTAIN CYTOTOXIC PROTOBERBERINE ALKALOIDS

被引：46

作者：

CUSHMAN, M ^{[1
]}

DEKOW, FW ^{[1
]}

JACOBSEN, LB ^{[1
]}

机构：

[1] PURDUE UNIV,SCH PHARM & PHARMACOL SCI,CELL CULTURE LAB,W LAFAYETTE,IN 47907

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 03期

关键词：

D O I：

10.1021/jm00189a025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The tetrahydroprotoberberine alkaloids 5 and 7 possessing a trans-quinolizidine conformation display in vitro KB cytotoxicities in contrast to their corresponding diastereomers 4 and 6 which exist in the cis-quinolizidine conformation and are much less toxic. The DNA-binding parameters of these compounds as well as the protoberberine salts 1, 8, and 9 have been examined by equilibrium dialysis. Only the quaternary salts bind to DNA. The alcohol 5 showed low in vivo activity against leukemia P388 systems, while the quaternary salts 8 and 9 proved to be toxic to the host. © 1979, American Chemical Society. All rights reserved.

引用

页码：331 / 333

页数：3

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