Cytotoxic acridinylthiourea and its platinum conjugate produce enzyme-mediated DNA strand breaks

被引：21

作者：

Brow, JM ^{[1
]}

Pleatman, CR ^{[1
]}

Bierbach, U ^{[1
]}

机构：

[1] Wake Forest Univ, Dept Chem, Winston Salem, NC 27109 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(02)00620-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The reactions of plasmid DNA modified with the novel acridinylthiourea, 1-[2-(acridin-9-ylamino)ethyl]-1,3-dimethylthiourea (1), and the corresponding intercalator-tethered platinum complex (2) with human type I and type II topoisomerases have been studied. Assays were based on evaluating DNA cleavage products resulting from incubations of drug-modified DNA in cell-free systems. 2 produces double-strand breaks in the presence of topo II while 1 proved to be a dual topo I/topo II poison. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2953 / 2955

页数：3

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