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Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme (2017)
Journal Article
Bharate, S. B., Chaudhuri, B., Vishwakarma, R. A., Jain, S. K., Sharma, R., Gatchie, L., & Williams, I. S. (2017). Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme. Bioorganic and Medicinal Chemistry Letters, 27(24), 5400-5403. https://doi.org/10.1016/j.bmcl.2017.11.013

© 2017 Elsevier Ltd The development of multi-drug resistance to existing anticancer drugs is one of the major challenges in cancer treatment. The over-expression of cytochrome P450 1B1 enzyme has been reported to cause resistance to cisplatin. With a... Read More about Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme.

(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 (2017)
Journal Article
Horley, N. J., Beresford, K. J., Kaduskar, S., Joshi, P., McCann, G. J., Ruparelia, K. C., …Chaudhuri, B. (2017). (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. Bioorganic and Medicinal Chemistry Letters, 27(24), 5409-5414. https://doi.org/10.1016/j.bmcl.2017.11.009

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... Read More about (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.

Biotransformation of Chrysin to Baicalein: Selective C6-Hydroxylation of 5,7-Dihydroxyflavone Using Whole Yeast Cells Stably Expressing Human CYP1A1 Enzyme (2017)
Journal Article
Bharate, S. B., Nuthakki, V. K., Williams, I. S., Chib, S., Gatchie, L., Joshi, P., …Chaudhuri, B. (2017). Biotransformation of Chrysin to Baicalein: Selective C6-Hydroxylation of 5,7-Dihydroxyflavone Using Whole Yeast Cells Stably Expressing Human CYP1A1 Enzyme. Journal of Agricultural and Food Chemistry, 65(34), 7440-7446. https://doi.org/10.1021/acs.jafc.7b02690

© 2017 American Chemical Society. Naturally occurring polyphenolic compounds are of medicinal importance because of their unique antioxidant, anticancer, and chemopreventive properties. Baicalein, a naturally occurring polyhydroxy flavonoid possessin... Read More about Biotransformation of Chrysin to Baicalein: Selective C6-Hydroxylation of 5,7-Dihydroxyflavone Using Whole Yeast Cells Stably Expressing Human CYP1A1 Enzyme.

Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines (2017)
Journal Article
Horley, N. J., Beresford, K. J., Chawla, T., McCann, G. J., Ruparelia, K. C., Gatchie, L., …Chaudhuri, B. (2017). Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines. European Journal of Medicinal Chemistry, 129, 159-174. https://doi.org/10.1016/j.ejmech.2017.02.016

© 2017 Elsevier Masson SAS The structure of alpha-napthoflavone (ANF), a potent inhibitor of CYP1A1 and CYP1B1, mimics the structure of chalcones. Two potent CYP1B1 inhibitors 7k (DMU2105) and 6j (DMU2139) have been identified from two series of syn... Read More about Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines.

Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance (2017)
Journal Article
Satti, N. K., Williams, I. S., Joshi, P., Gatchie, L., Sharma, M., Vishwakarma, R. A., …Bharate, S. B. (2017). Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance. Bioorganic and Medicinal Chemistry Letters, 27(16), 3683-3687. https://doi.org/10.1016/j.bmcl.2017.07.010

© 2017 Elsevier Ltd Inhibitors of CYP1 enzymes may play vital roles in the prevention of cancer and overcoming chemo-resistance to anticancer drugs. In this letter, we report synthesis of twenty-three pyrrole based heterocyclic chalcones which were s... Read More about Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance.