Synthesis And Antitumor Activity Evaluation Of Resveratrol Derivatives

Resveratrol is a natural antitoxin with polyphenol structure, mainly in the skin of grapes seed, red wine, mulberries, peanuts and other plants. It had a wide range of pharmacological activities, such as antitumor, anti-oxidation, anti-inflammatory, antibacterial, antiviral, cardiovascular protection and so on. But resveratrol had the disadvantages of more targets, low bioavailability and poor stability. So researchers are trying their best to find a novel of resveratrol derivatives of structural diversity, good selectivity, high activity and low toxicity.In this paper, we designed and synthesized two series of new resveratrol indanone and coumarin derivatives, based on the structure of (E)-1,3-dimethoxy-5-(4-methoxystyryl)benzene. The selected synthetic routes were simple, the raw materials were easy to obtain and the yields of compounds were high. The structures of the synthetic compounds were confirmed by 1H NMR,13C NMR, MS and elemental analysis.The method of MTT was used to test the anti-proliferative activities of resveratrol indanone and coumarin derivatives. The 19 resveratrol indanone derivatives had a good inhibitory activity for K562, U937, H1975, HeLa and HL60 cell lines. Among these compounds, the anti-proliferative activity of compound C11 was best. The IC50 values of compound C11 were 1.42 μM against DU145 cancer cell lines and the activities were stronger than the positive control TSA and Taxol.In addition, we also tested the anti-proliferative activities of resveratrol coumarin derivatives against A549, H1975, BGC-823 and Huh-7 cell lines. We found that compounds D2, D8 and D15 had a good inhibitory activity for Huh-7 cell line.We preliminary studied the structure-activity relationship of these compounds on the basis of the anti-proliferative activities and provided some theory for searching better activity of lead compounds for future.