Bioorganic chemistry

Design, synthesis, and evaluation of 4-(4′-aminobenzyl)-2-oxazolidinones as novel inhibitors of the cytochrome P-450 enzyme aromatase

S Ahmed, S Adat, A Murrells, CP Owen, Y Amanuel

Index: Ahmed, Sabbir; Adat, Shaheen; Murrells, Annabel; Owen, Caroline P.; Amanuel, Yonas Bioorganic Chemistry, 2002 , vol. 30, # 5 p. 315 - 331

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Citation Number: 7

Abstract

The synthesis of a series of N-alkylated 4-(4′ aminobenzyl)-2-oxazolidinones is described using a synthetically useful scheme which avoids the use of phosgene—since the derivatization is undertaken with the oxazolidin-2-one ring intact. The compounds were tested for human placental aromatase (AR) inhibition in vitro, using [1β, 2β-3H] androstenedione as substrate for the AR enzyme. The compounds were found, in general, ...