Bioorganic Chemistry p. 315 - 331 (2002)
Update date:2022-07-30
Topics:
Ahmed, Sabbir
Adat, Shaheen
Murrells, Annabel
Owen, Caroline P.
Amanuel, Yonas
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, to be more potent than the standard compound, amino-glutethimide (AG), and as such proved to be good lead compounds in the search for more specific AR inhibitors.
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