| 白桦酸衍生物的设计合成及抗肿瘤活性 |
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| 引用本文： | 朱梓菲,汤佳,王婷婷,陈莉.白桦酸衍生物的设计合成及抗肿瘤活性[J].中国药科大学学报,2012,43(5):395-400. |
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| 作者姓名： | 朱梓菲 汤佳 王婷婷 陈莉 |
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| 作者单位： | 中国药科大学天然药物化学教研室;中国药科大学天然药物化学教研室;中国药科大学天然药物化学教研室;中国药科大学天然药物化学教研室 |
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| 基金项目： | 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） |
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| 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。
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| 关 键 词： | 白桦酸 呋咱氮氧化物类 合成 硝酸酯 抗肿瘤活性 |
Synthesis and anti-tumor activity of novel betulinic acid derivatives |
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| ZHU Zi-fei,TANG Ji,WANG Ting-ting and CHEN Li.Synthesis and anti-tumor activity of novel betulinic acid derivatives[J].Journal of China Pharmaceutical University,2012,43(5):395-400. |
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| Authors: | ZHU Zi-fei TANG Ji WANG Ting-ting and CHEN Li |
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| Institution: | Department of Natural Medicinal Chemistry,China Pharmaceutical University,Nanjing 210009,China |
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| 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. |
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| Keywords: | betulinic acid(BA) furoxan synthesis nitrate anti-tumor activity |
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