8-羟基喹啉-7-醛缩酰肼席夫碱的绿色合成及抗肿瘤活性研究  

Green Synthesis and Antitumor Activities of 8-Hydroxyquinoline-7-carboxyaldehyde Aroylhydrazone Schiff Bases

作　　者：时蕾[1] 刘艳春[1] 王振平[1] 张贵生[1] 

机构地区：[1]绿色化学介质与反应教育部重点实验室河南师范大学化学与环境科学学院,新乡453007

出　　处：《化学通报》2013年第1期72-76,共5页Chemistry

基　　金：国家自然科学基金项目(21172056);“长江学者”和创新团队发展计划项目(IRT1061);河南省科学厅科技攻关项目(092102310115)资助

摘　　要：以水为反应介质,微波辐射促进8-羟基-7-喹啉甲醛与取代芳酰肼的缩合反应,制备了15种喹啉酰腙席夫碱化合物。反应在15～30min内完成,收率较高、后处理操作简便。化合物结构经1H NMR、13CNMR、IR和高分辨质谱确证。初步抗肿瘤活性测试结果表明,在20μg/mL浓度下,部分化合物对细胞周期分裂蛋白25B(CDC 25B)抑制率达到90%以上,具有潜在的抗肿瘤活性。Fifteen kinds of 8-hydroxyquinoline aroylhydrazone Schiff bases were synthesized by the condensation of 8-hydroxyquinoline-7-carboxyaldehyde and aryl hydrazines in neat water under microwave irradiation.The reactions were completed in 15~30min and the products were obtained in excellent isolated yields after simple operation.Their structures were confirmed by 1H NMR,13C NMR,IR and HRMS（ESI）.The results of preliminary antitumor activity tests indicated that some of the as-prepared compounds had greater than 90% inhibitory rate against cyclin CDC 25B in 20μg/mL,which mean they have potential antitumor activity.

关 键 词：8-羟基喹啉-7-醛席夫碱 微波辐射 绿色合成 抗肿瘤活性 

分 类 号：TQ463.5[化学工程—制药化工]