Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors |
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| Institution: | 1. College of Chemistry and Material Science, Hengyang Normal University, Key Laboratory of Functional Organometallic Materials of Hengyang Normal University, College of Hunan Province, Hengyang, Hunan 421008, People''s Republic of China;2. Faculty of Materials Science and Chemical Engineering, Ningbo University, Ningbo 315211, People''s Republic of China;1. Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University, 1-1 Gakuen-cho, Nakaku, Sakai, Osaka 599-8531, Japan;2. Department of Bioscience and Informatics, Graduate School of Life and Environmental Science, Osaka Prefecture University, 1-1 Gakuen-cho, Nakaku, Sakai, Osaka 599-8531, Japan;1. Faculty of Engineering, Shinshu University, Wakasato, Nagano 380-8533, Japan;2. Fujikoshi Machinery Corporation, 1650 Kiyono Matsushiro-machi, Nagano 381-1233, Japan;1. Research Institute of Physical and Organic Chemistry, Southern Federal University, Rostov-on-Don 344090, Russia;2. Institute of General and Inorganic Chemistry, Russian Academy of Sciences, Moscow 119991, Russia;3. Southern Scientific Center, Russian Academy of Sciences, Rostov-on-Don 344006, Russia;4. Southern Federal University, Faculty of Chemistry, Rostov-on-Don 344090, Russia |
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| Abstract: | The design and synthesis of isoxazole 3 is described, a potent JNK inhibitor with two fold selectivity over p38. Optimization of this scaffold led to compounds 27 and 28 which showed greatly improved selectivity over p38 by maintaining the JNK3 potency of compound 3. Extensive SAR studies will be described as well as preliminary in vivo data of the two lead compounds. |
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| Keywords: | JNK Kinase c-Jun Isoxazole |
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