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

DOI: 10.1016/S0960-894X(98)00305-9

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1741 - 1744 (1998)

Update date:2022-07-29

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Authors:

Lee Lee

Palmer Palmer

Wilson Wilson

Denny Denny

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Article abstract of DOI:10.1016/S0960-894X(98)00305-9

A four-step synthesis of 5-[N,N-bis(2-chloroethyl)amino]-1-methyl-2- nitroimidazole from 1-methyl2-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.

Full text of DOI:10.1016/S0960-894X(98)00305-9

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