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多卡霉素和CC - 1065的CBI类似物的DNA结合亚基中取代基效应的建立。

Establishment of substituent effects in the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065.

作者信息

Parrish Jay P, Kastrinsky David B, Stauffer Frederic, Hedrick Michael P, Hwang Inkyu, Boger Dale L

机构信息

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

出版信息

Bioorg Med Chem. 2003 Aug 15;11(17):3815-38. doi: 10.1016/s0968-0896(03)00194-9.

DOI:10.1016/s0968-0896(03)00194-9
PMID:12901927
Abstract

An extensive series of CBI analogues of the duocarmycins and CC-1065 exploring substituent effects within the first indole DNA binding subunit is detailed. In general, substitution at the indole C5 position led to cytotoxic potency enhancements that can be >/=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

详细介绍了一系列广泛的多卡霉素和CC - 1065的CBI类似物，这些类似物探索了第一个吲哚DNA结合亚基内的取代基效应。一般来说，在吲哚C5位置进行取代会导致细胞毒性效力增强，增强倍数可达1000倍以上，从而提供了含有单个DNA结合亚基的简化类似物，这些类似物比CBI - TMI、多卡霉素SA或CC - 1065更具效力（IC(50)=2 - 3 pM）。

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