Semi-synthesis and anti-proliferative activity evaluation of novel analogues of Honokiol.
Luo Y, Xu Y, Chen L, Hu J, Peng C, Xie D, Shi J, Huang W, Xu G, Peng M, Han J, Li R, Yang S, Wei Y.
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.