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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
【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.
【Key words】 Quinoxaline; 1,2,3-Trizoles; Synthesis; Anti-tumor activity;
- 【文献出处】 化学通报 ,Chemistry , 编辑部邮箱 ,2018年09期
- 【分类号】O626;TQ460.1
- 【被引频次】2
- 【下载频次】250