论文部分内容阅读
根据骨架迁跃原理,设计并合成了一系列具有酪氨酸激酶抑制剂拉帕替尼(Lapatinib)和诺拉替尼(Neratinib)结构片段的水杨酰芳胺类化合物,其结构均经IR,1H NMR,13C NMR和MS确证.采用四甲基偶氮唑盐(MTT)法考察所合成化合物的体外抗肿瘤细胞(A549,MCF-7,SGC-7901,Bel-7402)活性.结果表明,所合成的化合物对4种肿瘤细胞增殖均有一定的抑制活性,部分化合物的活性强于阳性对照药吉非替尼(Gefitinib).
A series of salicyloyl arylamines with the tyrosine kinase inhibitors Lapatinib and Neratinib have been designed and synthesized according to the theory of skeletal migration. The structures of the compounds are characterized by IR, 1H NMR, 13C NMR and MS.The inhibitory activities of the synthesized compounds against A549, MCF-7, SGC-7901 and Bel-7402 cells in vitro were investigated by MTT method.The results showed that The synthesized compounds have certain inhibitory activity on the proliferation of four kinds of tumor cells, and some compounds are more active than the gefitinib positive control drug.