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) 0045-2068Full text not available from this archive.
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.
|Uncontrolled Keywords:||molecular modeling perspective, mechanism|
|Faculty, School or Research Centre:||Faculty of Science (until 2011) > School of Pharmacy and Chemistry|
|Depositing User:||Automatic Import Agent|
|Date Deposited:||10 Mar 2010 14:37|
|Last Modified:||08 Apr 2011 15:26|
Actions (Repository Editors)
|Item Control Page|