263392-92-3Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of cyclic and acyclic nitrobenzylphosphoramide mustards for E. coli nitroreductase activation
Jiang, Yongying,Han, Jiye,Yu, Chengzhi,Vass, Simon O.,Searle, Peter F.,Browne, Patrick,Knox, Richard J.,Hu, Longqin
, p. 4333 - 4343 (2007/10/03)
In efforts to obtain anticancer prodrugs for antibody-directed or gene-directed enzyme prodrug therapy using E. coli nitroreductase, a series of nitrobenzylphosphoramide mustards were designed and synthesized incorporating a strategically placed nitro gro
Nitroaryl phosphoramide compositions and methods for targeting and inhibiting undesirable cell growth or proliferation
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Page 15, (2010/02/09)
The present invention relates to nitroaryl-substituted phosphoramide prodrug compounds and methods of producing the same for use in targeting and inhibiting undesirable cell growth or proliferation.
Nitroaryl Phosphoramides as Novel Prodrugs for E. coli Nitroreductase Activation in Enzyme Prodrug Therapy
Hu, Longqin,Yu, Chengzhi,Jiang, Yongying,Han, Jiye,Li, Zhuorong,Browne, Patrick,Race, Paul R.,Knox, Richard J.,Searle, Peter F.,Hyde, Eva I.
, p. 4818 - 4821 (2007/10/03)
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.
