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Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents

School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China
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Authors to whom correspondence should be addressed.
These authors contributed equally to the work.
Molecules 2018, 23(3), 515; https://doi.org/10.3390/molecules23030515
Received: 13 January 2018 / Revised: 11 February 2018 / Accepted: 14 February 2018 / Published: 26 February 2018
(This article belongs to the Section Medicinal Chemistry)
A series of bakuchiol derivatives were synthesized and evaluated for their anti-proliferative and the inhibitory activities on SMMC7721 cell line migration using PX-478 as a positive control. The results showed (S,E)-4-(7-methoxy-3,7-dimethyl-3-vinyloct-1-en-1-yl)phenol (10) to have the best activity among the tested compounds, which included PX-478. In addition, compound 10 showed greater inhibitory activity than that of bakuchiol in the transwell migration and invasion assays at every dose. In western blotting tests, compound 10 showed a promising ability to downregulate the expression of HIF-1α and its associated downstream proteins MMP-2 and MMP-9. Moreover, this effect was dose-dependent and could represent a possible mechanism of action for the anticancer activity of compound 10. View Full-Text
Keywords: bakuchiol derivatives; semi-synthesis; cytotoxicity; migration; invasion bakuchiol derivatives; semi-synthesis; cytotoxicity; migration; invasion
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MDPI and ACS Style

Wu, C.-Z.; Liu, D.-C.; Guo, X.; Dai, Y.; Ma, T.; Li, H.-M.; Huo, Q. Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents. Molecules 2018, 23, 515.

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