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

  • Eur J Med Chem. 2007 Feb;42(2):263-7. doi: 10.1016/j.ejmech.2006.08.006.
Xian-Feng Huang  1 ,  Ban-Feng Ruan ,  Xiao-Ting Wang ,  Chen Xu ,  Hui-Ming Ge ,  Hai-Liang Zhu ,  Ren-Xiang Tan
Affiliations
  • 1. Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
PMID: 17000031 DOI: 10.1016/j.ejmech.2006.08.006
Abstract

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.