DNA ALKYLATION PROPERTIES OF THE DUOCARMYCINS - (+)-DUOCARMYCIN-A, EPI-(+)-DUOCARMYCIN-A, ENT-(-)-DUOCARMYCIN-A AND EPI,ENT-(-)-DUOCARMYCIN-A

被引：80

作者：

BOGER, DL

YUN, WY

TERASHIMA, S

FUKUDA, Y

NAKATANI, K

KITOS, PA

JIN, Q

机构：

[1] SAGAMI CHEM RES CTR, SAGAMIHARA, KANAGAWA 229, JAPAN

[2] UNIV KANSAS, DEPT BIOCHEM, LAWRENCE, KS 66045 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(00)80407-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A study of the comparative in vitro cytotoxic activity and DNA alkylation properties of both enantiomers of the two diastereomers of (+)-duocarmycin A are detailed. The DNA alkylation efficiency and in vitro cytotoxic potency of the natural enantiomers ((+)-duocarmycin A > epi-(+)-duocarmycin A, 3-8x) exceed those of the unnatural enantiomers (ent-(-)-duocarmycin A, epi,ent-(-)-duocarmycin A) by at least 100x.

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页码：759 / +

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