| 李泳坤,李玖零,王恒山,王迎春.化学通报,2018,81(9):847-852. |
| 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 |
| 投稿时间：2018-04-06 修订日期：2018-06-10 |
| DOI： |
| 中文关键词: 喹喔啉 1,2,3-三唑 合成，抗肿瘤活性 |
| 英文关键词:Quinoxaline, 1,2,3-Trizoles, Synthesis, Anti-tumor activity |
| 基金项目:国家自然科学基金项目（21762017），湖南省自然科学基金( 2016JJ4075)，湖南省教育厅自然科学基金（16B211） |
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| 中文摘要: |
| 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、13C NMR 和HRMS 确证。初步体外抗肿瘤活性测试表明，目标化合物具有一定的抗肿瘤活性。 |
| 英文摘要: |
| Quinoxalines and 1,2,3-triazoles are both skeletons with wide biological activities. In this report, based on the combination principles of drug design, starting from o-phenylene diamine, phenylacetylene and organic azides, a series of new quinoxaline-triazole derivatives (3a～3n) 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 1HNMR, 13CNMR and HRMS. The result?of?preliminary bioassay?shows that?the target compounds?possess antitumor?activities?to some extent. |
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