Hypoxia activated prodrugs of a 9-aza-anthrapyrazole derivative that has promising anticancer activity

MH El-Dakdouki, N Adamski, L Foster…

Index: El-Dakdouki, Mohammad H.; Adamski, Nicholas; Foster, Lecia; Hacker, Miles P.; Erhardt, Paul W. Journal of Medicinal Chemistry, 2011 , vol. 54, # 23 p. 8224 - 8227

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Citation Number: 6

Abstract

Mono-and bis-N-oxides of a 9-aza-anthrapyrazole derivative having two 2-(dimethylamino) ethyl appendages were prepared by using a mild oxaziridine reagent. Biochemical and cell culture assays indicate that the bis-oxide is an inactive prodrug that readily converts to the active parent molecule under hypoxic conditions that are analogous to those present within certain tumors.