Synthesis and biochemical evaluation of analogs of aminoglutethimide based on phenylpyrrolidine-2, 5-dione

MJ Daly, GW Jones, PJ Nicholls, HJ Smith…

Index: Daly; Jones; Nicholls; Smith; Rowlands; Bunnett Journal of Medicinal Chemistry, 1986 , vol. 29, # 4 p. 520 - 523

Full Text: HTML

Citation Number: 39

Abstract

A series of (aminophenyl) pyrrolidine-2, 5-diones has been prepared that bear structural similarities to aminoglutethimide (I, 3-(4-aminophenyl)-3-ethylpiperidine-2, 6-dione). The inhibitory activity of these compounds was evaluated toward human placental aromatase and bovine adrenal cholesterol side chain cleavage (CSCC) enzyme assay systems. Selective, competitive inhibition of the aromatase enzyme system was demonstrated by 5 ( ...