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通过三尖杉碱α-酮酸酯与相应的溴代乙酸酯进行Reformatsky反应,合成了在侧链甲酯部分具有不同烷基结构的5个脱氧三尖杉酯碱衍生物。动物试验结果表明甲酯部分的甲基被其它烷基取代导致活性丧失。这又一次说明这类化合物抗癌活性的结构专属性较强。
Through the Reformatsky reaction of octreotide c-α-ketoacid with the corresponding bromoacetate, 5 deoxyharringtonine derivatives with different alkyl structures in the side chain methyl ester were synthesized. Animal test results show that the methyl part of the methyl group is replaced by other alkyl results in the loss of activity. This again shows that the anticancer activity of these compounds is structurally specific.