Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents.

Wu, Cheng-Zhu; Liu, Da-Chuan; Guo, Xing; Dai, Yiqun; Ma, Tao; Li, Hong-Mei; Huo, Qiang

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.

TERPENES synthesis; ANTINEOPLASTIC agents; CELL lines; CELL migration inhibition; CELL-mediated cytotoxicity; PSORALEA; LEGUMES; THERAPEUTICS

Molecules, 2018, Vol 23, Issue 3, p515

1420-3049

Academic Journal

10.3390/molecules23030515