Hh. Lee et al., SYNTHESIS AND HYPOXIA-SELECTIVE CYTOTOXICITY OF A 2-NITROIMIDAZOLE MUSTARD, Bioorganic & medicinal chemistry letters, 8(13), 1998, pp. 1741-1744
A four-step synthesis of bis(2-chloroethyl)amino]-1-methyl-2-nitroimid
azole from 1-methyl-2-nitroimidazole is described. This compound showe
d similar hypoxia-selective cytotoxicity to the dinitrobenzamide musta
rd SN 23862 in UV4 cells (ca. 40-fold), and superior selectivity (>7-f
old) in repair-competent AA8 cells. (C) 1998 Elsevier Science Ltd. All
rights reserved.