Author/Authors :
Charles F. Schwender، نويسنده , , Scott A. Beers، نويسنده , , Elizabeth A. Malloy، نويسنده , , Jacqueline J. Cinicola، نويسنده , , David J. Wustrow، نويسنده , , Keith D. Demarest، نويسنده , , Jerold Jordan، نويسنده ,
Abstract :
A series of α-substituted benzylphosphonic acids is described as inhibitors of human prostatic acid phosphatase, an enzyme which has been used as a model to study aryl phosphatases. The most potent inhibitors in this series are 2-trifluoromethylbenzhydrylphosphonic acid (9 μM), and α-(2-phenylethyl)benzylphosphonic acid (14 μM). The structure-activity studies suggest that bulk tolerance beyond the phosphate binding area limits the steric or hydrophobic contribution to inhibitor potency achieved through α-carbon substitution.
