【摘要】 对异甜菊醇C-环、D-环进行结构修饰与改造,同时将其C₁₉-COOH成酯,设计并合成了9个未见文献报道的新化合物（5¹3）,所有目标化合物的结构均经ESI-MS,IR,¹H NMR确定。采用MTT法测试了目标化合物对HCT116,Huh7,SW620及Hep G2等细胞的抗肿瘤活性。初步研究结果表明,化合物13表现出对人结肠癌HCT116细胞具有选择性抑制作用(IC₅₀=3.57μmol/L),与阳性对照舒尼替尼（sunitininb）(IC₅₀=5.62μmol/L)活性相当,化合物10对HCT116,Huh7,SW620均有较强抑制作用。更多还原

【Abstract】 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.更多还原