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Synthesis and hypoxia-selective cytotoxicity of a 2-nitroimidazole mustard
H H Lee1, B D Palmer, W R Wilson
1Auckland Cancer Society Research Centre, New Zealand.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
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 23,862 in UV4 cells (ca. 40-fold), and superior selectivity (> 7-fold) in repair-competent AA8 cells.