| 烟曲霉素生物素标记衍生物的合成及体外测试 |
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| 引用本文： | 刘芳,万军庭,陈少鹏,陆鑫,王新宇,周国春.烟曲霉素生物素标记衍生物的合成及体外测试[J].世界科技研究与发展,2010,32(5):699-701,722. |
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| 作者姓名： | 刘芳 万军庭 陈少鹏 陆鑫 王新宇 周国春 |
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| 作者单位： | [1]兰州大学生命科学学院细胞生物学研究所,兰州730000 [2]中国科学院广州生物医药与健康研究院,广州510530 |
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| 基金项目： | 国家自然科学基金，973重大研究计划 |
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| 摘 要： | 为了深入研究烟曲霉素及其衍生物的作用机理，合成了烟曲霉素的生物素标记衍生物6。化合物6是以辛二胺为连接臂通过酰胺键和氨基甲酸酯键把烟曲霉素的衍生物Fumagillol（compound2）和生物素连接而成，各中间体和目标化合物均经^1HNMR、^13CNMRMS表征，结构正确。体外活性测试结果表明目标化合物6可以高效的并且细胞选择性的抑制人脐静脉内皮细胞（HUVEC）增殖。体外受体结合实验证明化合物6与人甲硫氨酸氨肽酶-2（MetAP2）有很高的亲和力。
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| 关 键 词： | 烟曲霉素 抗血管生成 生物素标记衍生物 |
Synthesis and in Vitro Test of a Biotinylated Fumagillin Derivative |
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| LIU Fang,WAN Junting,CHEN Shaopeng,LU Xin,WANG Xinyu,ZHOU Guochun.Synthesis and in Vitro Test of a Biotinylated Fumagillin Derivative[J].World Sci-tech R & D,2010,32(5):699-701,722. |
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| Authors: | LIU Fang WAN Junting CHEN Shaopeng LU Xin WANG Xinyu ZHOU Guochun |
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| Institution: | 1. School of Life Sciences, Lanzhou University, Lanzhou 730000; 2. Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530) |
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| Abstract: | In order to further explore the mechanisms of fumagillin and its derivatives, A biotinylated fumagillin derivative of compound 6 is synthesized. It is linked by urethane bonds and amide bonds between fumagillol （2） and D-biotin. Its structures of target and intermediate compounds are confirmed by MS, ^1 H-NMR and ^13C-NMR. With the in vitro activity test,the objective compound （6） showed excellent cell selectivity and inhibition activity against the proliferation of HUVEC. In vitro reeeptor-binding assay,compound 6 has a high binding affinity of Methionine aminopeptidase 2 （ MetAP2）. |
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| Keywords: | fumagillin anti-angiogenesis biotinylated derivative |
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