白桦酸衍生物的设计合成及抗肿瘤活性

Synthesis and anti-tumor activity of novel betulinic acid derivatives

摘要: 以白桦酸（BA）为先导物，将BA的28-位-COOH通过不同的连接基团与硝酸酯或呋咱氮氧化物等NO供体偶联，合成了11个目标化合物。其结构均经IR，MS及¹H NMR确证；采用MTT法测定了所有目标物对人肝癌HepG2细胞和鼠黑色素瘤B16细胞的抑制活性。结果表明，多数呋咱氮氧化物类BA衍生物对肝癌HepG2细胞及鼠黑色素瘤B16细胞具有较强的抑制作用，活性值得进一步深入研究。

Abstract: A series of novel derivatives of betulinic acid(BA)-nitrate and BA-furoxan hybrids were synthesized by coupling NO donors with BA via various linkers.The compounds were structurally characterized by IR,MS and ¹H NMR,and their anti-tumor activity was determined in human hepatocellular carcinoma HepG2 cells and murine melanoma B16 cells by MTT assay.The preliminary results indicated that BA-furoxan conjugates exhibited stronger cytotoxic activity than BA in HepG2 and B16 cells and were worthy of further investigation.