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

Ahmed, Sabbir, Adat, Shaheen, Murrells, Annabel, Owen, Caroline P and Amanuel, Yonas (2002) Design, synthesis, and evaluation of 4-(4'-aminobenzyl)-2-oxazolidinones as novel inhibitors of the cytochrome P-450 enzyme aromatase. Bioorganic Chemistry, 30(5), pp. 315-331. ISSN (print) 0045-2068

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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 [1beta,2beta-3H]androstenedione as substrate for the AR enzyme. The compounds were found, in general, to be more potent than the standard compound, aminoglutethimide (AG), and as such proved to be good lead compounds in the search for more specific AR inhibitors.

Item Type: Article
Uncontrolled Keywords: molecular modeling perspective, mechanism
Research Area: Chemistry
Faculty, School or Research Centre: Faculty of Science (until 2011) > School of Pharmacy and Chemistry
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Depositing User: Automatic Import Agent
Date Deposited: 10 Mar 2010 14:37
Last Modified: 08 Apr 2011 15:26
URI: http://eprints.kingston.ac.uk/id/eprint/7186

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