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.
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。
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