【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（compound 2）和生物素连接而成,各中间体和目标化合物均经¹HNMR、¹³C NMR、MS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。更多还原

【Abstract】 In order to further explore the mechanisms of fumagillin and its derivatives, A biotinylated lumagillin derivative of compound 6 is synthesized.It is linked by urethane bonds and amide bonds between fumagilloi （2） and D-biotin.Its structures of target and intermediate compounds are confirmed by MS,¹H-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 receptor-binding assay,compound 6 has a high binding affinity of Methionine aminopeptidase 2 （ MetAP2）.更多还原