【摘要】：目的開發(fā)新的含芳香氮芥席夫堿化合物并考察其抗腫瘤活性。方法設(shè)計了系列含芳香氮芥的新席夫堿化合物(1~4),通過~1HNMR、~(13)C NMR、HRMS、FT-IR等對其結(jié)構(gòu)進行表征,并探討目標(biāo)化合物3的最佳合成條件:以乙醇做溶劑,1,4-丁二胺與4-二(2-氯乙基)氨基-2-羥基苯甲醛投料比(摩爾比)為1:2,80℃條件下回流反應(yīng)2h,產(chǎn)率在76%以上。用MTT法測定目標(biāo)化合物對A549(人肺腺癌細胞)和HepG2(人源肝癌細胞)的體外抗腫瘤活性。結(jié)果成功合成了4個新的含芳香氮芥席夫堿化合物。體外抗腫瘤活性結(jié)果表明,化合物1和2對兩種受試細胞株均表現(xiàn)出優(yōu)于臨床藥物美法侖的細胞毒性。而化合物1、2和3對HePG2細胞株的細胞毒性均表現(xiàn)出優(yōu)于臨床藥物美法侖的細胞毒性。結(jié)論設(shè)計合成的新含芳香氮芥席夫堿化合物1和2具有體外抗腫瘤活性的潛在優(yōu)勢,P$得進一步研究。
[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，

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