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Nitroaryl Phosphoramides as Novel Prodrugs for E. coli Nitroreductase Activation in Enzyme Prodrug Therapy

Lookup NU author(s): Professor Paul RaceORCiD


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Cyclic and acyclic nitroaryl phosphoramide mustard analogues were activated by E. coli nitroreductase, an enzyme explored in GDEPT. The more active acyclic 4-nitrobenzyl phosphoramide mustard (7) showed 167 500x selective cytotoxicity toward nitroreductase-expressing V79 cells with an IC50 as low as 0.4 nM. This is about 100x more active and 27x more selective than CB1954 (1). The superior activity was attributed to its better substrate activity (kcat/Km 19x better than 1) and/or excellent cytotoxicity of phosphoramide mustard released.

Publication metadata

Author(s): Hu L, Yu C, Jiang Y, Han J, Li Z, Browne P, Race PR, Knox RJ, Searle PF, Hyde EI

Publication type: Article

Publication status: Published

Journal: Journal of Medicinal Chemistry

Year: 2003

Volume: 46

Issue: 23

Pages: 4818-4821

Print publication date: 06/11/2003

Online publication date: 10/10/2003

ISSN (print): 0022-2623

ISSN (electronic): 1520-4804

Publisher: American Chemical Society


DOI: 10.1021/jm034133h

PubMed id: 14584930


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