摘要
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。
Ethyl 6-( furan-2-ylmethyleneamino)-2-methyl-1 H-indole-3-carboxylate was synthesized via three-step reaction using2,4-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,1 HNMR,13 CNMR and MS.Growth inhibitory activity of 6-( furan-2-ylmethyleneamino)-2-methyl-1 H-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.
出处
《化学试剂》
北大核心
2017年第11期1165-1168,1232,共5页
Chemical Reagents