Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065

被引：14
|
作者：
Boger, DL
Stauffer, F
Hedrick, MP
机构：
[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
[2] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 15期
基金：
美国国家卫生研究院;
关键词：
D O I：
10.1016/S0960-894X(01)00372-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of CBI analogues of the duocarmycins and CC-1065 exploring substituent effects within the first indole DNA binding subunit are detailed. Substitution at the indole C5 position led to cytotoxic potency enhancements that are greater than or equal to 1000-fold, providing simplified analogues containing a single DNA binding subunit that are more potent (IC50 = 2-3 pM) than CBI-TMI, duocarmycin SA, or CC-1065. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2021 / 2024
页数：4
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