Phosphatase inhibitors—III. Benzylaminophosphonic acids as potent inhibitors of human prostatic acid phosphatase

…, DA Loughney, E Malloy, K Demarest, J Jordan

Index: Beers, Scott A.; Schwender, Charles F.; Loughney, Deborah A.; Malloy, Elizabeth; Demarest, Keith; Jordan, Jerold Bioorganic and Medicinal Chemistry, 1996 ,  vol. 4,  # 10  p. 1693 - 1701

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Citation Number: 85

Abstract

Further investigation of the structural requirements of a series of benzylphosphonic acid inhibitors of human prostatic acid phosphatase has led to the highly potent series of α- aminobenzylphosphonic acids. The α-benzylaminobenzylphosphonic acid, with an IC50= 4 nM, exhibited a 3500-fold improvement in potency over the carbon analogue, α-phenylethyl. The enhanced potency may be due to a combination of four favorable interactions ...