Inhibition of retinoic acid metabolising enzymes by 2-(4-aminophenylmethyl)-6-hydroxy-3,4-dihydronaphthalen-1(2H)-one and related compounds

Journal of Enzyme Inhibition and Medicinal Chemistry
Andrew J KirbyClaire Simons

Abstract

In a search for inhibitors of all-trans retinoic acid (RA)-metabolising enzymes as potential agents for the treatment of skin conditions and cancer we have examined 2-(4-aminophenylmethyl)-6-hydroxy-3,4-dihydronaphthalen-1(2H)-one (5). Compound (5) is a moderate inhibitor of RA-metabolising enzymes in mammalian cadaverous tissue microsomes and homogenates as well as RA-induced enzymes in cultured human genital fibroblasts and HaCat cells. Overall (5) was more potent than or equipotent with ketoconazole, a standard inhibitor, in the cadaverous systems but less active towards the RA-induced cell culture systems. Examination of the data suggests that RA-induction generates metabolising enzymes not present in the cadaverous systems, which are more susceptible to inhibition by ketoconazole than (5).

Citations

Jan 28, 2010·Expert Opinion on Drug Metabolism & Toxicology·Francesca Marotta, Gian Mario Tiboni
Mar 15, 2006·Bioorganic & Medicinal Chemistry·Vincent C O NjarJyoti Patel
Jul 9, 2008·Journal of Enzyme Inhibition and Medicinal Chemistry·Stephane PautusClaire Simons
Dec 25, 2003·Journal of Enzyme Inhibition and Medicinal Chemistry·V P GreerC Simons
Aug 13, 2020·Journal of Enzyme Inhibition and Medicinal Chemistry·Yue SunYun Hou
May 1, 2021·International Journal of Molecular Sciences·Beata TylińskaAnna Janicka-Kłos

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