3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors |
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Authors: | Jiang Rong Duckett Derek Chen Weiming Habel Jeff Ling Yuan Yuan LoGrasso Philip Kamenecka Theodore M |
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Affiliation: | Department of Medicinal Chemistry, Scripps Florida, 5353 Parkside Drive, RF-2, Jupiter, FL 33458, USA. rjiang@scripps.edu |
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Abstract: | 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. |
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