Lookup NU author(s): Dr Caroline Bridgens,
Professor Gareth Veal,
Dr Chris Redfern,
Dr Jane Renwick
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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.
Author(s): Gomaa MS, Bridgens CE, Aboraia AS, Veal GJ, Redfern CPF, Brancale A, Armstrong JL, Simons C
Publication type: Article
Publication status: Published
Journal: Journal of Medicinal Chemistry
Print publication date: 23/03/2011
ISSN (print): 0022-2623
ISSN (electronic): 1520-4804
Publisher: American Chemical Society
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