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本文引用的文献

1
One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation.一种新型喹喔啉衍生物作为一种有效的人亲环素A抑制剂，对小鼠脾细胞增殖显示出高度抑制活性。
Bioorg Med Chem. 2006 Aug 15;14(16):5527-34. doi: 10.1016/j.bmc.2006.04.026. Epub 2006 May 6.
2
Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines.一些新型合成取代喹喔啉的合成及其抗原生动物活性
Bioorg Med Chem Lett. 2006 Feb 15;16(4):815-20. doi: 10.1016/j.bmcl.2005.11.025. Epub 2005 Nov 23.
3
Design, synthesis, and AMPA receptor antagonistic activity of a novel 6-nitro-3-oxoquinoxaline-2-carboxylic acid with a substituted phenyl group at the 7 position.一种新型的在7位带有取代苯基的6-硝基-3-氧代喹喔啉-2-羧酸的设计、合成及AMPA受体拮抗活性
Bioorg Med Chem. 2005 Oct 15;13(20):5841-63. doi: 10.1016/j.bmc.2005.05.030.
4
Rhodanine derivatives as inhibitors of JSP-1.作为JSP-1抑制剂的若丹宁衍生物
Bioorg Med Chem Lett. 2005 Jul 15;15(14):3374-9. doi: 10.1016/j.bmcl.2005.05.034.
5
Controlled microwave heating in modern organic synthesis.现代有机合成中的可控微波加热。
Angew Chem Int Ed Engl. 2004 Nov 26;43(46):6250-84. doi: 10.1002/anie.200400655.
6
Microwave-enhanced medicinal chemistry: a high-speed opportunity for convenient preparation of protease inhibitors.微波增强药物化学：便捷制备蛋白酶抑制剂的高速机遇。
Curr Opin Drug Discov Devel. 2004 Jul;7(4):417-27.
7
A new family of quinoline and quinoxaline analogues of combretastatins.一种新的秋水仙碱喹啉和喹喔啉类似物家族。
Bioorg Med Chem Lett. 2004 Jul 16;14(14):3771-4. doi: 10.1016/j.bmcl.2004.04.098.
8
Microwave - assisted chemistry in drug discovery.药物研发中的微波辅助化学
Curr Top Med Chem. 2004;4(7):773-92. doi: 10.2174/1568026043451078.
9
Quinoxaline chemistry. Part XVII. Methyl [4-(substituted 2-quinoxalinyloxy) phenyl] acetates and ethyl N-([4-(substituted 2-quinoxalinyloxy) phenyl] acetyl) glutamates analogs of methotrexate: synthesis and evaluation of in vitro anticancer activity.喹喔啉化学。第十七部分。甲氨蝶呤类似物甲基[4-(取代的2-喹喔啉氧基)苯基]乙酸酯和N-([4-(取代的2-喹喔啉氧基)苯基]乙酰基)谷氨酸乙酯：体外抗癌活性的合成与评价
Farmaco. 2004 Mar;59(3):185-94. doi: 10.1016/j.farmac.2003.11.014.
10
Quinoxalin-2-ones. Part 5. Synthesis and antimicrobial evaluation of 3-alkyl-, 3-halomethyl- and 3-carboxyethylquinoxaline-2-ones variously substituted on the benzo-moiety.喹喔啉-2-酮。第5部分。苯并部分上具有不同取代基的3-烷基-、3-卤甲基-和3-羧乙基喹喔啉-2-酮的合成与抗菌活性评估
Farmaco. 2003 Dec;58(12):1251-5. doi: 10.1016/S0014-827X(03)00198-8.

通过微波加速亲核取代反应制备6-取代喹喔啉JSP-1抑制剂

Preparation of 6-substituted quinoxaline JSP-1 inhibitors by microwave accelerated nucleophilic substitution.

作者信息

Zhang Li, Qiu Beiying, Li Xin, Wang Xin, Li Jingya, Zhang Yongliang, Liu Jian, Li Jia, Shen Jingkang

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.

出版信息

Molecules. 2006 Dec 21;11(12):988-99. doi: 10.3390/11120988.

DOI:10.3390/11120988
PMID:18007403
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6148675/
Abstract

A small library of 6-aminoquinoxalines has been prepared by nucleophilic substitution of 6-fluoroquinoxaline with amines and nitrogen-containing heterocycles under computer-controlled microwave irradiation. Some compounds were found to be potent inhibitors of JNK Stimulatory Phosphatase-1 (JSP-1) in an in vitro biological assay.

摘要

通过在计算机控制的微波辐射下，用胺类和含氮杂环对6-氟喹喔啉进行亲核取代反应，制备了一个由6-氨基喹喔啉组成的小型文库。在体外生物学试验中，发现一些化合物是JNK刺激磷酸酶-1（JSP-1）的有效抑制剂。