Synthesis and Cytotoxicity Evaluation of Panaxadiol Derivatives
OBJECTIVE To obtain stronger cytotoxic activity of panaxadiol derivatives.METHODS The 3-amino panaxadiol was prepared by the bioelectronic isosteric principle,and then 18 derivatives of cinnamic acid,NO donor and other types of panaxadiol derivatives were synthesized,among them,12 compounds had not been reported in the literature,and their structures had been confirmed by 1H-NMR,13C-NMR and mass spectrometry.These compounds were evaluated for their cytotoxic activity by MTS assay against human leukemia cell line HL-60,liver cancer cell line SMMC-7721,lung cancer cell line A-549,breast cancer cell line MCF-7,and colon cancer cell line SW480.RESULTS These results showed that compounds 6c,7 as well as 7j exhibited potent inhibitory activities against all five tumor cells,especially the IC50 values of compound 7 against HL-60 and SMMC-7721cells were 3.41 and 4.51 μmol·L-1,respectively.It was significantly superior to panaxadiol in cytotoxicity.CONCLUSION These results show that 7 and 7j can be used as promising lead compounds for further research.
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