Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest

• Main Authors: Zhen-Hui Xin, Hui-Hui Yang, Yu-Han Gan, Ya-Li Meng, Ya-Peng Li, Li-Ping Ge, Cun-Hui Zhang, Lian-Na Liu, Yan-Fei Kang
• Format: Article
• Language: English
• Published: Elsevier 2020-07-01
• Series: Journal of Pharmacological Sciences
• Subjects: Resveratrol; Cell apoptosis; Cell cycle arrest
• Online Access: http://www.sciencedirect.com/science/article/pii/S1347861320300347

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.