2-Nitroimidazole dual-function bioreductive drugs: studies on the effects of regioisomerism and side-chain structural modifications on differential cytotoxicity and …

…, MD Threadgill, P Webb, IJ Stratford…

Index: Naylor, Matthew A.; Threadgill, Michael D.; Webb, Paul; Stratford, Ian J.; Stephens, Miriam A.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 19 p. 3573 - 3578

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Citation Number: 18

Abstract

(RSU-1069, 1) is the most effective of a large number of nitroheterocyclic compounds that have been synthesized and evaluated as radiosensitizers and bioreductively-activated cyt~ toxins.~-~ Compounds of this type owe their selective cytotoxicity toward hypoxic cells within tumors to their bioreductive properties. Activation in vivo is by anaerobic enzymatic reduction to toxic metabolite^.^ The radiosensitizing activity of 2-nitroimidazoles is via fast ...