Effect of C2/C3-endo unsaturation on the cytotoxicity and DNA-binding reactivity of pyrrolo[2,1-c][1,4]benzodiazepines

被引：22

作者：

Gregson, SJ

Howard, PW

Barcella, S

Nakamya, A

Jenkins, TC

Kelland, LR

Thurston, DE

机构：

[1] Univ Portsmouth, Sch Pharm & Biomed Sci, CRC Gene Targeted Drug Design Res Grp, Portsmouth PO1 2DT, Hants, England

[2] Univ Bradford, Canc Res Grp, Yorkshire Canc Res Lab Drug Design, Bradford BD7 1DP, W Yorkshire, England

[3] Inst Canc Res, CRC Ctr Canc Therapeut, Sutton SM2 5PX, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(00)00350-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel C2/C3-endo unsaturated pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) has been synthesised via cleavage of the N10-Alloc protecting group from appropriate precursors. Biophysical and biological evaluations show that the presence of C2/C3-endo unsaturation ill the PBD C-ring enhances both DNA-binding reactivity and in vitro cytotoxic potency. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1849 / 1851

页数：3

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