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(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.
Horley NJ, Beresford KJM, Kaduskar S, Joshi P, McCann GJP, Ruparelia KC, Williams IS, Gatchie L, Sonawane VR, Bharate SB, Chaudhuri B. Horley NJ, et al. Among authors: williams is. Bioorg Med Chem Lett. 2017 Dec 15;27(24):5409-5414. doi: 10.1016/j.bmcl.2017.11.009. Epub 2017 Nov 6. Bioorg Med Chem Lett. 2017. PMID: 29138024
CYP enzymes, expressed within live human suspension cells, are superior to widely-used microsomal enzymes in identifying potent CYP1A1/CYP1B1 inhibitors: Identification of quinazolinones as CYP1A1/CYP1B1 inhibitors that efficiently reverse B[a]P toxicity and cisplatin resistance.
Sonawane VR, Siddique MUM, Gatchie L, Williams IS, Bharate SB, Jayaprakash V, Sinha BN, Chaudhuri B. Sonawane VR, et al. Among authors: williams is. Eur J Pharm Sci. 2019 Apr 1;131:177-194. doi: 10.1016/j.ejps.2019.02.016. Epub 2019 Feb 15. Eur J Pharm Sci. 2019. PMID: 30776468
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