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Synthesis of melphalan derivatives and their antitumor activities
Author(s): 
Pages: 115-119
Year: Issue:  2
Journal: World Phytomedicines

Keyword:  melphalanmatrine18α-glycyrrhetinic acidantitumor activity;
Abstract: Objective To design and synthesize melphalan derivatives by combining the matrine and 18α-Glycyrrhetinic acid to melphalan, and to evaluate their antitumor activities in vitro and in vivo. Methods Sophocarpine and melphalan were used as starting materials to synthesize the melphalan derivative 2 by addition and acylation reaction; 18α-Glycyrrhetinic acid and melphalan were used as starting materials to synthesize the melphalan derivative 5 by esterification and acylation reaction. The target compounds were characterized by elemental analyses, MS and 1H-NMR. The antitumor activities in vitro were evaluated by MTT method. Anti-tumor experiments in vivo were also done for the compound 2 displaying high activities in vitro. Results The total yield of target compound 2 and 5 were 21.3% and 18.1%. The in vitro antitumor activity experiments showed that the antitumor activity of target compound 2 was higher than those of compound 5, 18α-glycyrrhetinic acid, matrine and melphalan. The inhibition rates of tumor growth of compound 2 with 6 and 9 μmol/kg were 52.00% and 62.12%, while the inhibition rate of tumor growth of melphalan with 6 μmol/kg was 39.93%. The inhibition effect of tumor growth of compound 2 is better than that of melphalan, especially in high dose. Conclusion The compound 2 exhibits high antitumor activity in vitro and in vivo, which could be valuable for further development.
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