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Semi-synthetic honokiol analogues prepared by modifying 5- and/or 3′-position(s) exhibited improved anti-proliferative potencies and displayed more potent anti-drug resistance effects on cisplatin-resistant A2780 human ovarian carcinoma cells.
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.