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

作　　者：朱梓菲[1] 汤佳[1] 王婷婷[1] 陈莉[1] 

机构地区：[1]中国药科大学天然药物化学教研室,南京210009

出　　处：《中国药科大学学报》2012年第5期395-400,共6页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.2097210);中国药科大学先声药业研究生创新基金项目(No.CX10S-006XS);中国药科大学大学生实践创新训练项目(2009)~~

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。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.

关 键 词：白桦酸 呋咱氮氧化物类 合成 硝酸酯 抗肿瘤活性 

分 类 号：R914.5[医药卫生—药物化学]