Nitroarylhydroxymethylphosphonic acids as inhibitors of CD45

…, R Brosius, JL Pellegrino-Gensey, J Siekierka

Index: Beers, Scott A.; Malloy, Elizabeth A.; Wu, Wei; Wachter, Michael P.; Gunnia, Uma; Cavender, Druie; Harris, Crafford; Davis, Janet; Brosius, Ruth; Pellegrino-Gensey, J. Lee; Siekierka, John Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 12 p. 2203 - 2211

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Citation Number: 27

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