A novel approach to the synthesis of cytotoxic C2-C3 unsaturated pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) with conjugated acrylyl C2-substituents

被引：19

作者：

Chen, ZZ ^{[1
]}

Gregson, SJ ^{[1
]}

Howard, PW ^{[1
]}

Thurston, DE ^{[1
]}

机构：

[1] Canc Res UK Gene Targeted Drug Design Res Grp, Dept Pharmaceut & Biol Chem, Sch Pharm, London WC1N 1AX, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 06期

关键词：

PBDs; DNA binding; cytotoxic; SAR;

D O I：

10.1016/j.bmcl.2003.12.094

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A concise synthesis of three novel C2-C3 unsaturated pyrrolo[2,1-c][1,4]benzodiazepine analogues (18-20) containing conjugated acrylyl C2-substituents is reported that utilises Heck coupling to install the C2-acrylyl side chains. These analogues possess significant cytotoxicity according to the NO 60-cell line screen with 18 surpassing anthramycin (1) in potency. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1547 / 1549

页数：3

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