Synthesis and antitumor activity of isosteviol derivatives

To explore isosteviol derivatives with more potent antitumor activity, nine novel C-ring and/or D-ring modified compounds( 5 - 13 )were designed and synthesized. The structures of the derivatives were identified by IR, 1H NMR and MS. Cytotoxicity of all the target compounds was tested by MTT method in HepG2, HCT116, Huh7 and SW620 cells, and the preliminary results showed that compound 13 exhibited a selective cytotoxicity(IC₅₀=3. 57 μmol/L)against HCT116 cell, and was comparable to that of sunitininb(IC₅₀=5. 62 μmol/L). Compound 10 has good inhibitory effects on HCT116, Huh7, SW620 cell lines.