M. Tercel et al., A NOVEL NITROSUBSTITUTED SECO-CI - APPLICATION AS A REDUCTIVELY ACTIVATED ADEPT PRODRUG, Bioorganic & medicinal chemistry letters, 6(22), 1996, pp. 2741-2744
An alternative synthesis of seco-CI alkylating agents bearing a nitrog
en substituent at C-6 is reported. The nitro compound 3 prepared by th
is route exhibits a 400-fold increase in cytotoxicity against UV4 cell
s in the presence of a nitroreductase enzyme from Escherichia coli B,
suggesting it as a potential prodrug for use in antibody-directed enzy
me prodrug therapy. Copyright (C) 1996 Elsevier Science Ltd