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Small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26): Synthesis and biological evaluation of imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates

Gomaa, Mohamed Sayed, Bridgens, Caroline E., Aboraia, Ahmed, Veal, Gareth J., Redfern, Christopher P. F., Brancale, Andrea, Armstrong, Jane L. and Simons, Claire 2011. Small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26): Synthesis and biological evaluation of imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates. Journal of Medicinal Chemistry 54 (8) , pp. 2778-2791. 10.1021/jm101583w

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Abstract

The synthesis and potent inhibitory activity of novel imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates in a MCF-7 CYP26A1 microsomal assay is described. The induction of CYP26A1 mRNA was used to evaluate the ability of the compounds to enhance the biological effects of all-trans retinoic acid (ATRA) in a retinoid-responsive neuroblastoma cell line. The most promising inhibitor, 3-imidazol-1-yl-2-methyl-3-[4-(naphthalen-2-ylamino)-phenyl]-propionic acid methyl ester (20), with an IC50 of 3 nM (compared with liarozole IC50 of 540 nM and R116010 IC50 of 10 nM) was further evaluated for CYP selectivity using a panel of CYP enzymes, mutagenicity (Ames screen), and hepatic stability.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
Publisher: American Chemical Society
ISSN: 0022-2623
Last Modified: 02 Jun 2019 22:51
URI: http://orca-mwe.cf.ac.uk/id/eprint/7451

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