Objective: To synthesize the novel derivatives with the natural resource 18α-glycyrrhetinic acid and evaluate their antitumor activity. Method: The novel 18α-glycyrrhetinic acid derivatives (7 and 8) were synthesized by combining the matrine and nitrogen mustard melphalan with the 18α-glycyrrhetinic acid. The target compounds were characterized by 1H-NMR

MS and elemental analyses. Their antitumor activities against SMMC-7721 cell lines and their toxicities on normal BRL cell lines were evaluated by MTT assay in vitro. Result: The compound 7 exhibited a higher antitumor activity and nontoxicity in vitro. In the in vivo test in mice

with the dose of 6

9 μmol·kg-1

the inhibition rates of compound 7 in HepA tumor growth were 40.72% and 60.12%

which were higher than parent drug. Meanwhile

with the dose of 6 μmol·kg-1

the inhibition rate of melphalan was 39.93%. Conclusion: The compound 7 exhibited a high antitumor activity against hepatoma cells

which is worth further studying and developing.