Cytotoxic acridinylthiourea and its platinum conjugate produce enzyme-mediated DNA strand breaks |
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| Authors: | Brow Jennifer M Pleatman Cynthia R Bierbach Ulrich |
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| Affiliation: | Department of Chemistry, Wake Forest University, Winston-Salem, NC 27109, USA. |
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| Abstract: | 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. |
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