A novel design strategy for stable metal complexes of nitrogen mustards as bioreductive prodrugs

…, C Evans, DJ Robins, CC O'Hare…

Index: Parker, Laurie L.; Lacy, Stephen M.; Farrugia, Louis J.; Evans, Cameron; Robins, David J.; O'Hare, C. Caroline; Hartley, John A.; Jaffar, Mohammed; Stratford, Ian J. Journal of Medicinal Chemistry, 2004 , vol. 47, # 23 p. 5683 - 5689

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Citation Number: 51

Abstract

Tumor hypoxia provides a key difference between healthy and cancerous cells. It can be exploited to produce drug selectivity, offering a reductase-rich environment for prodrug activation. Nitrogen mustard drugs are cytotoxic, but usually unselective. Polyamine mustards are candidates for conversion into hypoxia-selective prodrugs via complexation with metals. Reduction to a less stable complex can free the active drug. The novel Cu (II) ...