Literature DB >> 9459018

Nitroarylhydroxymethylphosphonic acids as inhibitors of CD45.

S A Beers1, E A Malloy, W Wu, M P Wachter, U Gunnia, D Cavender, C Harris, J Davis, R Brosius, J L Pellegrino-Gensey, J Siekierka.   

Abstract

A series of nitroarylhydroxymethylphosphonic acids was synthesized and evaluated as inhibitors of CD45. It was discovered that both the alpha hydroxy and nitro groups are essential for activity. Potency is enhanced by the addition of a large lipophilic group on the aryl ring adjacent to the phosphonic acid moiety. Kinetics studies have shown that these compounds are competitive inhibitors and thus bind at the active site of this enzyme.

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Year:  1997        PMID: 9459018     DOI: 10.1016/s0968-0896(97)00174-0

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


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