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.
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)
出处
《化学通报》
CAS
CSCD
北大核心
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
关键词
喹喔啉
1
2
3-三唑
合成
抗肿瘤活性
Quinoxaline
1
2
3-Trizoles
Synthesis
Anti-tumor activity
