Bioorganic and Medicinal Chemistry p. 2203 - 2211 (1997)
Update date:2022-08-04
Topics:
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
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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