Synthesis of a heterocyclic aza-enediyne and its DNA-cleavage properties

被引：22

作者：

David, WM

Kumar, D

Kerwin, SM ^{[1
]}

机构：

[1] Univ Texas, Coll Pharm, Div Med Chem, Austin, TX 78712 USA

[2] Univ Texas, Inst Mol & Cellular Biol, Austin, TX 78712 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(00)00516-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The benzimidazolium salt 2, incorporating an aza-enediyne moiety, has been prepared and is shown to be a very effective DNA-cleavage agent under mild physiological conditions. Its mechanism of action is currently under investigation but may involve the generation of a diradical intermediate, DNA alkylation, or both. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：2509 / 2512

页数：4

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