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Some 1,2-diphenylethane derivatives as inhibitors of retinoic acid-metabolising enzymes

Greer, Valerie Patricia, Mason, Peter, Kirby, Andrew James, Smith, H., Nicholls, Paul Joseph and Simons, Claire 2003. Some 1,2-diphenylethane derivatives as inhibitors of retinoic acid-metabolising enzymes. Journal of Enzyme Inhibition and Medicinal Chemistry 18 (5) , pp. 431-443.

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In a search for novel inhibitors of RA-metabolising enzyme inhibitors as potential anti-cancer agents some 1,2-ethandiones, 2-hydroxyethanones and 1-ethylene-dioxyethanones based on aryl-substituted 1,2-diphenylethane have been examined. Several of the compounds were weak inhibitors of the non-specific rat liver microsomal P450 enzymes and moderate inhibitors of the RA-induced enzymes in cultured human genital fibroblasts, where the RA-specific enzyme CYP26 is probably expressed. The 2-hydroxy-ethanone (13) with a 1-(4-dimethylaminophenyl) substituent was overall the most potent compound for rat liver microsomal enzyme (IC50 = 52.1 μM; ketoconazole, 2.8 μM) and the RA-induced enzyme (100 μM, 65.9% inhibition; ketoconazole, 20 μM, 75.0%). Modification of the dimethylamino group in (13) with more hydrophobic dialkylamino functions or separate modification of the 2-(2,4-dichlorophenyl) function did not improve potency.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
Publisher: Informa Healthcare
ISSN: 1475-6366
Last Modified: 05 Aug 2020 15:14

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