Synthesis and hypoxia-selective cytotoxicity of A 2-nitroimidazole mustard

HH Lee, BD Palmer, WR Wilson, WA Denny

Index: Lee; Palmer; Wilson; Denny Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 13 p. 1741 - 1744

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Citation Number: 19

Abstract

A four-step synthesis of 5-[N, N-bis (2-chloroethyl) amino]-1-methyl-2-nitroimidazole from 1- methyl-2-nitroimidazole is described. This compound showed similar hypoxia-selective cytotoxicity to the dinitrobenzamide mustard SN 23862 in UV4 cells (ca. 40-fold), and superior selectivity (> 7-fold) in repaircompetent AA8 cells.