2. Academic Validation
  3. Synthesis and hypoxia-selective cytotoxicity of a 2-nitroimidazole mustard

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

  • Bioorg Med Chem Lett. 1998 Jul 7;8(13):1741-4. doi: 10.1016/s0960-894x(98)00305-9.
H H Lee 1,  B D Palmer,  W R Wilson,  W A Denny
Affiliations

Affiliation

  • 1 Auckland Cancer Society Research Centre, New Zealand.
PMID: 9873426 DOI: 10.1016/s0960-894x(98)00305-9
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.

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