A novel nitro-substituted seco-CI: application as a reductively activated ADEPT prodrug

M Tercel, WA Denny, WR Wilson

Index: Tercel; Denny; Wilson Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 22 p. 2741 - 2744

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Citation Number: 31

Abstract

An alternative synthesis of seco-Cl alkylating agents bearing a nitrogen substituent at C-6 is reported. The nitro compound 3 prepared by this route exhibits a 400-fold increase in cytotoxicity against UV4 cells in the presence of a nitroreductase enzyme from Escherichia coli B, suggesting it as a potential prodrug for use in antibody-directed enzyme prodrug therapy.