作为新型c-Jun氨基末端激酶抑制剂的3,5-二取代喹啉
3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.
作者信息
Jiang Rong, Duckett Derek, Chen Weiming, Habel Jeff, Ling Yuan Yuan, LoGrasso Philip, Kamenecka Theodore M
机构信息
Department of Medicinal Chemistry, Scripps Florida, 5353 Parkside Drive, RF-2, Jupiter, FL 33458, USA.
出版信息
Bioorg Med Chem Lett. 2007 Nov 15;17(22):6378-82. doi: 10.1016/j.bmcl.2007.08.054. Epub 2007 Aug 26.
The structure-based design and synthesis of a novel series of c-Jun N-terminal kinase (JNK) inhibitors with selectivity against p38 is reported. The unique structure of 3,5-disubstituted quinolines (2) was developed from the previously reported 4-(2,7-phenanthrolin-9-yl)phenol (1). The X-ray crystal structure of 16a in JNK3 reveals an unexpected binding mode for this new scaffold with protein.
报道了一系列对p38具有选择性的新型c-Jun氨基末端激酶（JNK）抑制剂的基于结构的设计与合成。3,5-二取代喹啉（2）的独特结构是由先前报道的4-(2,7-菲咯啉-9-基)苯酚（1）衍生而来。JNK3中16a的X射线晶体结构揭示了这种新支架与蛋白质的意外结合模式。
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