6-(呋喃-2-亚甲氨基)-2-甲基-1H-吲哚-3-羧酸乙酯的合成、表征与生物活性研究

以2,4-二硝基氯苯为原料,经过3步反应得到标题化合物。当温度为78℃,反应时间为8.5 h,目标化合物的收率可达65%。通过IR、1HNMR、13CNMR和MS光谱技术对其结构进行表征。运用SRB法评价了目标化合物对人体肺癌细胞的生长抑制活性。初步的生物实验表明,该化合物对癌细胞H1792、A549、H157和Calu-1具有生长抑制作用,且具有浓度依赖性。细胞周期分析发现其能诱导Calu-1细胞凋亡。

Synthesis,Characterization and Biological Activity of Ethyl 6-(Furan-2-ylmethyleneamino)-2-Methyl-1H-Indole-3-Carboxylate

Ethyl 6-(furan-2-ylmethyleneamino)-2-methyl-1H-indole-3-carboxylate was synthesized via three-step reaction using 2,4-dinitrochlorobenzene as the material.When the reaction temperature was 78 ℃ and reaction time was 8.5 h,the yield of target compound by the column chromatography reached 65％.The structure of compound was confirmed by IR,1HNMR,13CNMR and MS.Growth inhibitory activity of 6-(furan-2-ylmethyleneamino)-2-methyl-1H-indole-3-carboxylate on human lung cancer cells was evaluated by the method of SRB.The preliminary biological experiments showed that compound possessed growth inhibition activity to cancer cells H1792,A549,H157 and Calu-1 in a dosage dependent manner.It was found that compound induced apoptosis of Calu-1 cells by cell cycle analysis.