Probing for a hydrophobic a binding register in prostate-specific membrane antigen with phenylalkylphosphonamidates

…, TA Girtsman, LY Wu, JA Rowley, NM Santiago…

Index: Maung, Jack; Mallari, Jeremy P.; Girtsman, Teri A.; Wu, Lisa Y.; Rowley, Jennifer A.; Santiago, Nicholas M.; Brunelle, Alan N.; Berkman, Clifford E. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 18 p. 4969 - 4979

Full Text: HTML

Citation Number: 51

Abstract

To explore for the existence of an auxiliary hydrophobic binding register remote from the active site of PSMA a series of phenylalkylphosphonamidate derivatives of glutamic acid were synthesized and evaluated for their inhibitory potencies against PSMA. Both the phenyl- and benzylphosphonamidates (1a and 1b) exhibited only modest inhibitory potency against. The phenethyl analog 1c was intermediate in inhibitory potency while inhibitors ...