Synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) C8 cyclic amine conjugates

被引：25
作者：
Masterson, LA
Croker, SJ
Jenkins, TC
Howard, PW
Thurston, DE
机构：
[1] Univ London, Sch Pharm, Canc Res UK Gene Targeted Drug Design Res Grp, London WC1 1AX, England
[2] Univ Bradford, Tom Connors Canc Res Ctr, Yorkshire Canc Res Lab Drug Design, Bradford BD7 1DP, W Yorkshire, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 04期
关键词：
DNA binding; pyrrolobenzodiazepines; PBDs; sequence-selective; gene targeting;
D O I：
10.1016/j.bmcl.2003.12.017
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We report examples of a series of novel pyrrolo[2,1-c][1,4]benzodiazepine (PBD) analogues 12-15 prepared from a common functionalized building block 11 that can be conveniently synthesized on a large scale and in optically pure form. Isoindoline analogue 15 is the most cytotoxic agent in this series, has the highest DNA-binding affinity, and shows significant activity in the in vivo hollow fibre assay. (C) 2004 Elsevier Ltd. All rights reserved.
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页码：901 / 904
页数：4
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