HONG Ting, JIANG Wei, DONG Huai-Ming, QIU Sheng-Xiang, LU Yu. Synthesis and cytotoxic activities of E-resveratrol derivatives[J]. Chinese Journal of Natural Medicines, 2015, 13(5): 375-382.
Citation: HONG Ting, JIANG Wei, DONG Huai-Ming, QIU Sheng-Xiang, LU Yu. Synthesis and cytotoxic activities of E-resveratrol derivatives[J]. Chinese Journal of Natural Medicines, 2015, 13(5): 375-382.

Synthesis and cytotoxic activities of E-resveratrol derivatives

  • The present study was designed to synthesize derivatives of E-resveratrol and evaluate their cytotoxic activity in vitro. Different functional groups were conjugated with the phenolic hydroxyl group of E-resveratrol, and the double bond of E-resveratrol was reduced. The in vitro cytotoxicity of the synthetic derivatives was evaluated against three tumor cell lines (A549, LAC, and HeLa) using the MTT assay. Twenty-six E-resveratrol derivatives were synthesized and their structures were confirmed by 1H NMR, MS, IR, and elemental analyses. Compounds 1-6, 12, 15-21, and 23-26 were reported for the first time. Among them, Compounds 1, 2, 4, 5, and 9-11, showed significant cytotoxicity against tumor cells; especially, Compound 1 showed an IC50 value of 4.38 molL-1 in the A549 cells which was 15-fold more active than E-resveratrol; Compound 9 showed an IC50 value of 1.41 molL-1 in the HeLa cell line which was 90-fold more active than E-resveratrol, and close to adriamycin. The structure-activity relationships were also investigated. Compounds 1, 2 and 9-11 may serve as potential lead compounds for the discovery of new anticancer drugs.
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