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Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest
Zhen-Hui Xin1, Hui-Hui Yang1, Yu-Han Gan1
1Hebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of China.
Abstract:
Resveratrol has been extensively studied as the anti-cancer agent. A variety of resveratrol analogues have been developed with structural modification to improve its bioactivity. In this work, resveratrol analogues, compound 1-4, were designed and synthesized with the Stille-Heck reaction. These results showed compound 1-4 had better anticancer effect than that of parent resveratrol. Especially compound 1 ((E)-4,4'-(ethene-1,2-diyl)bis(3-methylphenol)) displayed the excellent cytotoxicity and high selectivity. The mechanism research indicated compound 1 inhibited cell proliferation by binary paths of cell cycle arrest in S phase regulated by cyclin A1/A2 and apoptosis induction mediated by Bax/Bcl2 in a prooxidant manner.
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