溴代去甲斑蝥素酰胺衍生物的合成和抗癌活性研究.

Objective To find a highly effective anti-cancer compound, to design and synthesize novel norcantharidin derivatives, and to test its anti-tumor activity. Methods Maleic anhydride was reacted with furan for obtaining the midhody 5,6-dihydrogen norcantharidin, then further reacted with liquid bromine for obtaining the midbody 5, 6-dibromo norcantharidin and ul-teriorly generated multiple bromo-substituted norcantharidin amide derivatives by the heating reflux reaction with multiple aromat­ic amines. The compounds C1,C2,C3,C5,C8 were performed the inhibiting activity test of human hepatoma HepG2 cells and human gastric cancer BGC803 cells by CCK-8 method. Results In the action at a concentration of 50 μmol/L, the proliferation inhibiting rate of 5 kinds of tested compounds on human hepatoma HepG2 cells was 48.20%, the minimum was 7.10%, the highest inhibiting rate of 4 kinds of tested compound on human gastric cancer BGC803 cells reached 64.23% ;the proliferation inhibiting rate on gastric cancer BGC803 cells reached more than 50.00%. Conclusion Bromo-substituted norcantharidin amide derivatives have a certain anti-gastric cancer activity, but its anti-hepatoma activity is relatively weak. [ABSTRACT FROM AUTHOR]