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

Affiliation

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.

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