Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 12, Issue 20, Pages 2953-2955Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00620-0
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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.
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