NOVEL NITROPHENYLAZIRIDINE COMPOUNDS AND THEIR USE AS PRODRUGS

摘要

A range of aziridin-1-yl nitrobenzamides (A-C) are provided for use as prodrugs in conjunction with nitroreductase (NR) enzymes. The amides may have 1 or 2 N-substituents which may be bulky and polar. For example, 5-(aziridin-1-yl) -N-[2-(4-morpholino) ethyl] -2,4-dinitrobenzamide of Compound (1) was found to be highly active against all NR+ cell lines tested.