Semi-synthesis and anti-proliferative activity evaluation of novel analogues of Honokiol

  • Bioorg Med Chem Lett. 2009 Aug 15;19(16):4702-5. doi: 10.1016/j.bmcl.2009.06.071.
Youfu Luo  1 ,  Yongbin Xu ,  Lijuan Chen ,  Jia Hu ,  Cheng Peng ,  DaChun Xie ,  Jianyou Shi ,  Wencai Huang ,  Guobin Xu ,  Ming Peng ,  Jing Han ,  Rui Li ,  Shengyong Yang ,  Yuquan Wei
Affiliations
  • 1. State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, PR China.
PMID: 19589678 DOI: 10.1016/j.bmcl.2009.06.071
Abstract

A series of honokiol analogues were synthesized by modifying the 5- and/or 3'-position(s) of honokiol to assess their anti-tumor effects. Some compounds exerted more potent anti-proliferative activities than those of honokiol on K562 leukemia cells, A549 alveolar basal epithelial cells, SPC-A1 adenocarcinoma cells and A2780 human ovarian carcinoma cells in vitro. Compounds 2b, 3a, and 3c displayed most potent anti-proliferative activities against these tested cell strains and their anti-drug resistance effects were evaluated in vitro on cisplatin-resistant A2780 human ovarian carcinoma cells. The structure-activity relationship was also proposed.