Hypoxia-selective antitumor agents. 8. Bis (nitroimidazolyl) alkanecarboxamides: a new class of hypoxia-selective cytotoxins and hypoxic cell radiosensitizers

…, WR Wilson, JW Moselen, BD Palmer…

Index: Hay; Wilson; Moselen; Palmer; Denny Journal of Medicinal Chemistry, 1994 , vol. 37, # 3 p. 381 - 391

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Citation Number: 69

Abstract

A series of novel bis (nitroimidazoly1) alkanecarboxamides has been prepared and evaluated for hypoxia-selective cytotoxicity and hypoxic cell radiosensitisation in vitro and in vivo. The compounds were prepared by direct coupling of preformed side chain acid and amine components, using diethyl phosphorocyanidate at room temperature. Although designed to be bis-bioreductive prodrugs of DNA cross-linking agents, none of the ...