A NOVEL NITROSUBSTITUTED SECO-CI - APPLICATION AS A REDUCTIVELY ACTIVATED ADEPT PRODRUG

Citation
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
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
6
Issue
22
Year of publication
1996
Pages
2741 - 2744
Database
ISI
SICI code
0960-894X(1996)6:22<2741:ANNS-A>2.0.ZU;2-7
Abstract
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