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 ORCID: https://orcid.org/0000-0002-9487-1100 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.

Full text not available from this repository.

Abstract

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:	19 Oct 2022 09:03
URI:	https://orca.cardiff.ac.uk/id/eprint/19825

Citation Data

Cited 10 times in Scopus. View in Scopus. Powered By Scopus® Data

Actions (repository staff only)

Edit Item