Discovery of Potent, Highly Selective, and Orally Bioavailable Pyridine Carboxamide c-Jun NH2-Terminal Kinase Inhibitors
Journal of Medicinal Chemistry2006Vol. 49(15), pp. 4455–4458
Citations Over TimeTop 10% of 2006 papers
Hongyu Zhao, Michael D. Serby, Zhili Xin, Bruce G. Szczepankiewicz, Mei Liu, Christi Kosogof, Bo Liu, Lissa T.J. Nelson, Eric F. Johnson, Sanyi Wang, Terry M. Pederson, Rebecca J. Gum, Jill E. Clampit, Deanna L. Haasch, Cele Abad‐Zapatero, Elizabeth H. Fry, Cristina M. Rondinone, James M. Trevillyan, Hing L. Sham, Gang Liu
Abstract
C-Jun NH2 terminal kinases (JNKs) are important cell signaling enzymes. JNK1 plays a central role in linking obesity and insulin resistance. JNK2 and JNK3 may be involved in inflammatory and neurological disorders, respectively. Small-molecule JNK inhibitors could be valuable tools to study the therapeutic benefits of inhibiting these enzymes and as leads for potential drugs targeting JNKs. In this report, we disclose a series of potent and highly selective JNK inhibitors with good pharmacokinetic profiles.
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