2-(吗啉基)氨基-N-吡喃基苯甲酰胺类VEGFR 2激酶抑制剂的合成及其抗肿瘤活性研究

Study on the synthesis and antitumor activity of 2- (morpholine) amino-N-pyran benzamide VEGFR 2 kinase inhibitors

摘要: VEGFR 2是一种重要的第五类血管内皮细胞生长因子受体,在新生血管形成中起关键作用,因此设计合成可选择性抑制VEGFR 2激酶的药物非常重要.实验过程中以索拉非尼为先导化合物,共设计了26个类似结构的目标分子,并合成出相应的目标化合物.实验过程中,还采用了MTT法对所合成的目标化合物进行了抗肿瘤生物活性研究,实验结果表明,其目标化合物对人肺癌细胞(H1975和A549)、人宫颈癌细胞(Hela)增殖都有一定的抑制活性.

Abstract: VEGFR 2 is an important receptor of the fifth class vascular endothelial growth factor ,and it has played a critical role in the formation of new blood vessels,so it is important to design and synthesize a drug to selectively inhibit VEGFR 2 kinase.Sorafenib as precursor compounds,a total of 26 target molecules with similar structures are designed,and the corresponding target compounds are also synthesized.In addition,MTT is adopted to study antitumor biological activity of the target compounds .The results show that the target compounds have some inhibitory activity to human lung cancer cell (H1975 and A549),human cervical cancer cells (Hela) proliferation.