N10-吖啶酮乙酸酯的合成及细胞毒活性研究  

Synthesis and cytotoxic activity study of N-acridone acetate

作　　者：刘改枝[1] 史礼君 刘萌芽 许杜娟 李金鑫 蔡邦荣 LIU Gai-zhi;SHI Li-jun;LIU Meng-ya;XU Du-juan;LI Jin-xin;CAI Bang-rong(College of Pharmacy,Henan University of Chinese Medicine,Zhengzhou 450046,China)

机构地区：[1]河南中医药大学药学院,河南郑州450046

出　　处：《中国药物化学杂志》2021年第7期498-503,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学青年基金项目(81803740);河南中医药大学博士基金项目(00104311-2019-33);河南省科技攻关项目(202102310514)。

摘　　要：目的设计合成具有良好抗肿瘤活性的吖啶酮类衍生物,并进行体外细胞毒活性研究。方法以吖啶酮为起始原料,根据药物设计的结构拼合原理,设计合成了7个吖啶酮乙酸酯类衍生物,通过1H-NMR、^(13)C-NMR和HR-MS谱对目标化合物的结构进行了确证,并采用MTT法测试了目标化合物对胃癌细胞的体外细胞毒活性。结果与结论设计合成的7个目标化合物均未见文献报道,其中化合物4c和4e对人胃癌细胞(SCG)表现出良好的细胞毒活性,IC50值分别为18.46、11.85μmol·L^(-1),具有进一步开发为新型抗肿瘤药物的潜力。It had been reported that acridones had a wide range of antitumor activities.The N10-acridone acetate were designed and synthesized, and their cytotoxic activities were evaluated.Seven acridone acetyl ester derivatives were designed and synthesized according to the principle of structure combination of pharmaceutical intermediate acridone.The structures of the target compounds were confirmed by 1H-NMR,^(13)C-NMR and HR-ESI-MS.The cytotoxicity of the synthesized compounds to gastric cancer cells was tested by MTT method.None of the seven target compounds had been reported, compound 4 c and 4 e showed better cytotoxicity against SGC gastric cancer cells with IC50 values of 18.46 μmol·L^(-1) and 11.85 μmol·L^(-1),respectively.

关 键 词：吖啶酮 抗肿瘤 细胞毒活性 合成 

分 类 号：R914[医药卫生—药物化学]