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.
Huang
Xian-Feng
XF
Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
Ruan
Ban-Feng
BF
Wang
Xiao-Ting
XT
Xu
Chen
C
Ge
Hui-Ming
HM
Zhu
Hai-Liang
HL
Tan
Ren-Xiang
RX
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007624:KB Cells; D000077185:Resveratrol; D013267:Stilbenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D013267:Stilbenes; D000077185:Resveratrol