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多卡霉素和CC - 1065的CBI类似物的DNA结合亚基内的取代基效应

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

作者信息

Boger D L, Stauffer F, Hedrick M P

机构信息

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

出版信息

Bioorg Med Chem Lett. 2001 Aug 6;11(15):2021-4. doi: 10.1016/s0960-894x(01)00372-9.

DOI:10.1016/s0960-894x(01)00372-9
PMID:11454471
Abstract

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 > or =1000-fold, providing simplified analogues containing a single DNA binding subunit that are more potent (IC(50)=2-3 pM) than CBI-TMI, duocarmycin SA, or CC-1065.

摘要

详细介绍了一系列探索第一个吲哚DNA结合亚基内取代基效应的双咔霉素和CC - 1065的CBI类似物。在吲哚C5位置进行取代导致细胞毒性效力增强超过或等于1000倍，从而提供了含有单个DNA结合亚基的简化类似物，其比CBI - TMI、双咔霉素SA或CC - 1065更具效力（IC(50)=2 - 3 pM）。

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