Synthesis and cytotoxic evaluation of a series of resveratrol derivatives modified in C2 position

Eleven C2-substituted derivatives of resveratrol (trans-3,4′,5-trihydroxystilbene, RES) were prepared by partial synthesis from RES and evaluated for their cytotoxic activities against a human nasopharyngeal epidermoid tumor cell line KB. Among them, compounds 2 and 3 were more active than 5-fluorouracil (5-FU), an anticancer drug, and compound 5f exhibited similar activity to 5-FU. On the basis of the biological results, structure–activity relationships were discussed.

Graphical abstractA series of resveratrol derivatives were prepared by the partial synthesis and evaluated for their cytotoxic activities against a human nasopharynyeal epidermoid tumor cell line KB.Figure optionsDownload full-size imageDownload as PowerPoint slide