喹喔啉-三唑衍生物的设计与合成及其抗肿瘤活性  

Design,Synthesis and Antitumor Activities of Quinoxaline-triazole Derivatives

作　　者：李泳坤 李玖零 王恒山 王迎春 Li Yongkun;Li Jiuling;Wang Hengshan;Wang Yingchun(College of Chemistry and Chemical Engineering,Hunan Engineering Laboratory for Analyse and Drugs Development of Ethnomedicine in Wuling Mountains,Jishou University,Jishou 416000;State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources,School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University,Guilin 541004)

机构地区：[1]吉首大学化学化工学院武陵山地区民族药解析与创制湖南省工程实验室,吉首416000 [2]广西师范大学化学与药学学院药用资源化学与药物分子工程重点实验室,桂林541004

出　　处：《化学通报》2018年第9期847-852,共6页Chemistry

基　　金：国家自然科学基金项目(21762017);湖南省自然科学基金项目(2016JJ4075);湖南省教育厅自然科学基金项目(16B211)资助

摘　　要：喹喔啉和1,2,3-三唑都是具有广泛生物活性的杂环结构母体。本文基于药物设计的拼合原理,以简单易得的邻苯二胺、苯乙炔及有机叠氮为原料,通过三组分"两步一锅法"将喹喔啉和1,2,3-三唑活性亚结构进行拼接,合成了一系列共14个新型喹喔啉-三唑衍生物(3a^3n)。该法操作简单,无需分离中间体,两步总产率52.6%~78.4%。合成的目标化合物结构经~1H NMR、^(13)C NMR和HRMS确证。初步体外抗肿瘤活性测试表明,合成的目标化合物具有一定的抗肿瘤活性。Quinoxalines and 1,2,3-triazoles are both skeletons with wide biological activities. In this paper,based on the combination principles of drug design,starting from o-phenylene diamine,phenylacetylene and organic azides,a series of new quinoxaline-triazole derivatives（ 3 a ～ 3 n） were synthesized by three-component ＂two step one-pot＂reactions. This pr℃edure had the advantages of operation simplicity and without isolating intermediates with isolated yields in the range of 52. 6% ～ 78. 4%. The structures of target compounds were characterized by ^1 H NMR,^13 C NMR and HRMS. The result of preliminary bioassay shows that the synthesized target compounds possess antitumor activities to some extent.

关 键 词：喹喔啉 1 2 3-三唑 合成 抗肿瘤活性 

分 类 号：O626[理学—有机化学] TQ460.1[理学—化学]