Synthesis and Biological Evaluation of 3??(Prop??2??enyl)??and 3??(Prop??2??ynyl) pyrrolidine??2, 5??dione Derivatives as Potential Aromatase Inhibitors

…, M Ahmadi, HJ Smith, PJ Nicholls

Index: Barrell; Woo; Ahmadi; Smith; Nicholls Journal of Pharmacy and Pharmacology, 1996 , vol. 48, # 2 p. 154 - 159

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Citation Number: 3

Abstract

Abstract 3-(4′-Aminophenyl) pyrrolidine-2, 5-dione (WSP3), a known reversible inhibitor of P450 aromatase, was modified using molecular graphics and our model of reversible inhibitor and substrate binding to resemble 10β-prop-2-ynylestr-4-ene-3, 17-dione (PED), a mechanism-based inactivator of the enzyme.