(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent.

Abstract

The overexpression of CYP1 family of enzymes is reported to be associated with development of human carcinomas. It has been well reported that CYP1A1 specific inhibitors prevents carcinogenesis. Herein, thirteen pyridine-4-yl series of chalcones were synthesized and screened for inhibition of CYP1 isoforms 1A1, 1B1 and 1A2 in Sacchrosomes™ and live human… (More)
DOI: 10.1016/j.bmcl.2017.11.009

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@article{Horley2017E3345Trimethoxyphenyl1pyridin4ylpro, title={(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent.}, author={Neill J Horley and Kenneth J M Beresford and Supriya Kaduskar and Prashant Joshi and Glen J P McCann and Ketan C. Ruparelia and Ibidapo Steven Williams and Linda Gatchie and Vinay R Sonawane and Sandip B Bharate and Bhabatosh Chaudhuri}, journal={Bioorganic & medicinal chemistry letters}, year={2017}, volume={27 24}, pages={5409-5414} }