Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) Inhibitors

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 de...

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Enregistré dans:
Détails bibliographiques
Publié dans:Bioorg Med Chem Lett
Auteurs principaux: He, Yuanjun, Duckett, Derek, Chen, Weimin, Ling, Yuan Yuan, Cameron, Michael D., Lin, Li, Ruiz, Claudia H., LoGrasso, Philip V., Kamenecka, Theodore M., Koenig, Marcel
Format: Artigo
Langue:Inglês
Publié: 2013
Sujets:
Article
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC4540177/
https://ncbi.nlm.nih.gov/pubmed/24332487
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2013.11.052
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