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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

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【作者】 李泳坤李玖零王恒山王迎春

【Author】 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;State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources,School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University;

【通讯作者】 王迎春;

【机构】 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

【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(3a3n)。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、13C 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。

【Abstract】 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 procedure 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
【Key words】 Quinoxaline1,2,3-TrizolesSynthesisAnti-tumor activity
【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
  • 【分类号】O626;TQ460.1
  • 【被引频次】2
  • 【下载频次】250
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