本文選題：喹啉衍生物 + 多靶點��； 參考：《中國新藥雜志》2016年13期

【摘要】：目的:合成一系列喹啉苯甲酰胺類衍生物(3a~3l,4a~4h)作為多靶點受體酪氨酸激酶抑制劑,并進行體外抗腫瘤活性研究。方法:以4,7-二氯喹啉和對氨基苯甲酸為起始原料,經(jīng)2步或3步反應合成目標化合物。采用四氮唑鹽(MTT)法測試目標化合物對A549,Eca-109,Hela這3種腫瘤細胞的抑制作用。結(jié)果:所合成的化合物中抑制活性最強為化合物4a,對Hela,Eca-109及A549細胞的IC50值分別為(1.04±0.12),(0.37±0.06),(2.16±1.05)μmol·L~(-1),對腫瘤細胞的抑制活性強于舒尼替尼(sunitinib)。結(jié)論:與舒尼替尼相比,本實驗中所涉及到化合物均表現(xiàn)出一定的抑制活性,這類喹啉苯甲酰胺類衍生物能夠作為多靶點受體酪氨酸激酶抑制劑進行深入研究。
[Abstract]:Aim: to synthesize a series of quinoline benzoyl amines as multitarget receptor tyrosine kinase inhibitors and to study their antitumor activity in vitro. Methods: the target compound was synthesized by two or three steps reaction of 4-4-dichloroquinoline and p-aminobenzoic acid. The inhibitory effects of the target compounds on A549 Eca-109 Hela tumor cells were measured by MTT method. Results: the inhibitory activity of the synthesized compounds was the strongest for 4 years, and the IC50 values of the two compounds were 1.04 鹵0.12, 0.37 鹵0.06 渭 mol / L, respectively, and the inhibitory activity on tumor cells was stronger than that on susunitinib. Conclusion: compared with sulnitinib, the compounds involved in this study have some inhibitory activities, and these quinoline benzoyl amines can be used as multi-target receptor tyrosine kinase inhibitors.
【作者單位】： 華僑大學分子藥物研究院;廣州優(yōu)米健醫(yī)藥科技有限公司;
【基金】：福建省自然科學基金資助項目(2015J01342) 泉州市科技計劃重點項目(Z1424024)
【分類號】：R914.5
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本文編號：1940730