新型含氮芥席夫碱化合物的合成及其抗肿瘤活性研究
发布时间：2018-10-25 12:10
【摘要】：目的开发新的含芳香氮芥席夫碱化合物并考察其抗肿瘤活性。方法设计了系列含芳香氮芥的新席夫碱化合物(1~4),通过~1HNMR、~(13)C NMR、HRMS、FT-IR等对其结构进行表征,并探讨目标化合物3的最佳合成条件:以乙醇做溶剂,1,4-丁二胺与4-二(2-氯乙基)氨基-2-羟基苯甲醛投料比(摩尔比)为1:2,80℃条件下回流反应2h,产率在76%以上。用MTT法测定目标化合物对A549(人肺腺癌细胞)和HepG2(人源肝癌细胞)的体外抗肿瘤活性。结果成功合成了4个新的含芳香氮芥席夫碱化合物。体外抗肿瘤活性结果表明,化合物1和2对两种受试细胞株均表现出优于临床药物美法仑的细胞毒性。而化合物1、2和3对HePG2细胞株的细胞毒性均表现出优于临床药物美法仑的细胞毒性。结论设计合成的新含芳香氮芥席夫碱化合物1和2具有体外抗肿瘤活性的潜在优势,P$得进一步研究。
[Abstract]:Objective to develop a new Schiff base compound containing aromatic nitrogen mustard and to investigate its anti-tumor activity. Methods A series of new Schiff base compounds containing aromatic nitrogen mustard were designed and characterized by ~ 1H NMR ~ (13) C NMR,HRMS,FT-IR. The optimum synthesis conditions of target compound 3 were discussed as follows: when ethanol was used as solvent, the molar ratio (molar ratio) of 1-butylamine to 4-bis (2-chloroethyl) amino-2-hydroxybenzaldehyde was 1: 280 鈩，
本文编号：2293662
[Abstract]:Objective to develop a new Schiff base compound containing aromatic nitrogen mustard and to investigate its anti-tumor activity. Methods A series of new Schiff base compounds containing aromatic nitrogen mustard were designed and characterized by ~ 1H NMR ~ (13) C NMR,HRMS,FT-IR. The optimum synthesis conditions of target compound 3 were discussed as follows: when ethanol was used as solvent, the molar ratio (molar ratio) of 1-butylamine to 4-bis (2-chloroethyl) amino-2-hydroxybenzaldehyde was 1: 280 鈩，
本文编号：2293662
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