3-取代喹喔啉衍生物的合成及其抗肿瘤活性的研究  

Study on synthesis and antitumour activities of 3-subsitituted quinoxaline derivatives

作　　者：张春玲[1] 许秀枝[1] 王艰[1] 杨州[1] 李柱来[1] 

机构地区：[1]福建医科大学药学院,福建福州350004

出　　处：《广东药学院学报》2013年第1期25-28,共4页Academic Journal of Guangdong College of Pharmacy

基　　金：福建省教育厅科技项目(JA11115);福建医科大学教授基金(JS10005)

摘　　要：目的合成3-取代喹喔啉衍生物,并研究其对细胞株K562和PANC-1的抗肿瘤活性。方法以邻苯二胺与1,2-二酮类化合物草酸二乙酯通过环合、氯代、亲核取代3步反应合成目标化合物;用MTT法测定目标化合物的抗肿瘤活性。结果合成了7个新的喹喔啉衍生物,经IR、1H-NMR表征确认结构,其中化合物6对K562细胞的抑制效果最佳,IC50值为0.836μmol.L-1。结论合成得到的7个新的3-取代喹喔啉衍生物,均有较好的体外抗肿瘤活性。Objective To synthetize 3-subsitituted quinoxaline derivatives and study their anti-tumor activities on cell K562 and PANC-1.Methods The compounds were synthesized with the reaction of 1,2-diaminobenzene and 1,2-dione compounds diethyl oxalate by cyclization,chloro and nucleophilic substitution.MTT method was used to evaluate antitumor activities of their compounds.Results Seven new compounds were synthesized and characterized by IR and ^1H-NMR.The inhibition ratio of Compound 6 on K562 cell was the best with IC50 0.836 μmol·L^-1.Conclusion Seven new 3-subsitituted quinoxaline derivatives were synthesized and had good antitumor activity in vitro.

关 键 词：喹喔啉 衍生物 合成 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学]