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Yao xue xue bao = Acta pharmaceutica Sinica 2012-Jan

[Synthesis and anti-tumor activity of paeonol and its derivatives].

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Xue-Jun Wang
Jian-Li Liu
Jiang-Kai Wang

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A series of paeonol derivatives have been synthesized by simple acylation and etherification of the paeonol. Anti-tumor activities of the synthesized compounds were evaluated against HeLa and MCF-7 cells lines in vitro by the standard MTT assay. It was found that the derivatives were more active against HeLa than MCF-7. The results also indicated that 4-methoxy group is the synergistic group of paeonol's anti-tumor activity and ketone carbonyl side chain is essential functional group of paeonol's anti-tumor activity. Compound 2d had stronger antiproliferative activities than paeonol against HeLa and MCF-7 cell lines with IC50 values of 2.67 and 4.74 micromol x L(-1) respectively. The results showed that paeonol derivatives were worth to be intensively studied further.

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