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Synthesis and Cytotoxic Evaluation of a Series of Resveratrol Derivatives

A total of 17 resveratrol (=(E)‐5‐[2‐(4‐hydroxyphenyl)ethenyl]benzene‐1,3‐diol) derivatives were synthesized from resveratrol (RES) through a facile approach. Among them, 13 compounds, 2 and 6–17, were reported for the first time, while 1 and 3–5 had already been reported several years ago. The cytotoxic activities of these compounds were evaluated against human nasopharyngeal epidermoid tumor cell line KB, and compounds 1 and 8–11 showed strong anticancer activities in vitro, comparable with that of 5‐fluorouracil, an anticancer drug. On the basis of the experimental data obtained, structure–activity relationships are discussed.