Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Cheng-Zhu WuQiang Huo

Abstract

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.

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Citations

Jan 16, 2019·Contact Dermatitis·Laura MalinauskieneAnželika Chomičiene

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Methods Mentioned

BETA
xenografts
NMR
column chromatography
silica gel column chromatography

Software Mentioned

SPSS

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