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- W2978091090 abstract "3077 The bisdioxopiperazines dexrazoxane and levrazoxane are strong catalytic inhibitors of mammalian DNA topoisomerase II. The individual stereoisomers of their platinum(II) complexes, cis-PtCl2(dexrazoxane) and cis-PtCl2(levrazoxane), were synthesized and their structures were determined by x-ray crystallography. Dexrazoxane and levrazoxane inhibit cell growth because they inhibit topoisomerase II, whereas cisplatin acts through the formation of DNA cross-links. It was hypothesized that platinum(II) complexes of dexrazoxane and levrazoxane would retain both activities and yield drugs with a dual mode of action. Both cis-PtCl2(dexrazoxane) and cis-PtCl2(levrazoxane) inhibited Chinese hamster ovary cell growth, but more weakly than dexrazoxane and levrazoxane did. Based on the inability of these platinum complexes to inhibit the catalytic activity of topoisomerase II it was concluded that these compounds did not inhibit cell growth by. targeting topoisomerase II. The recent x-ray structure of dexrazoxane bound to the ATPase region of a yeast topoisomerase II has been used to model the platinum complexes into the bisdioxopiperazine binding site. A comparison of the conformation of cis-PtCl2(dexrazoxane) to that of dexrazoxane bound to the dimer interface of topoisomerase II showed that the highly constrained cis-PtCl2(dexrazoxane) was in a highly unfavorable conformation for binding. Also neither of the platinum complexes were able to cross-link DNA. Thus the cell growth inhibitory activity of these complexes were also not likely due to any cisplatin-type cross-linking activity. Support: CIHR and a Canada Research Chair in Drug Development." @default.
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- W2978091090 date "2004-04-01" @default.
- W2978091090 modified "2023-09-24" @default.
- W2978091090 title "Synthesis and characterization of the biological activity of the cisplatin analogs cis-PtCl2(dexrazoxane) and cis-PtCl2(levrazoxane) of the topoisomerase II inhibitors dexrazoxane (ICRF-187) and levrazoxane (ICRF-186)." @default.
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