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Synthesis and CYP26A1 inhibitory activity of 1-[benzofuran-2-yl-(4-alkyl/aryl-phenyl)-methyl]-1H-triazoles and amino-benzooxazole derivatives [Abstract]

Pautus, Stephane Mathieu, Coogan, Michael Peter and Simons, Claire 2007. Synthesis and CYP26A1 inhibitory activity of 1-[benzofuran-2-yl-(4-alkyl/aryl-phenyl)-methyl]-1H-triazoles and amino-benzooxazole derivatives [Abstract]. Abstracts of Papers - American Chemical Society 233 , p. 636.

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Abstract

All-trans-retinoic acid (atRA) has shown spectacular success in the treatment of cancer and leukaemia, however atRA is rapidly metabolised by the P450 enzyme CYP26. Two series of CYP26 inhibitors were synthesised: a series of 4-alkyl/aryl-substituted 1-[benzofuran-2-yl-phenylmethyl]-1H-triazoles and a series of amino-benzooxazole derivatives. The triazole derivatives were prepared using a method previously described by our group. The amino-benzooxazole derivatives were envisaged from a docking experiment using a CYP26A1 homology model (based on CYP3A4) template. The molecular docking of the amino-benzooxazole imidazole derivatives indicated multiple hydrogen bonding in addition to coordination between the imidazole nitrogen and the P450 haem transition metal. The triazole derivatives were evaluated for CYP26A1 inhibitory activity using a MCF-7 cell-based assay. The 4-ethyl and the 4-phenyl-1,2,4-triazole derivatives displayed inhibitory activity (IC50 4.5 and 7 ìM respectively) comparable with liarozole (IC50 7 ìM). The synthesis, molecular modelling and inhibitory CYP26 inhibitory activity of the novel compounds will be presented.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RM Therapeutics. Pharmacology
Additional Information: 7:00 PM-9:00 PM, Sunday, March 25, 2007 Hyatt Regency Chicago -- Riverside Center, Poster
Publisher: American Chemical Society
Last Modified: 04 Jun 2017 03:20
URI: http://orca-mwe.cf.ac.uk/id/eprint/19838

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