Discovery of Potent, Highly Selective, and Orally Bioavailable Pyridine Carboxamide c-Jun NH2-Terminal Kinase Inhibitors
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- 作者：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 Pederson ; Rebecca J. Gum ; Jill E. Clampit
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：July 27, 2006
- 年：2006
- 卷：49
- 期：15
- 页码：4455 - 4458
- 全文大小：112K
- 年卷期：v.49,no.15(July 27, 2006)
- ISSN：1520-4804
文摘
C-Jun NH2 terminal kinases (JNKs) are important cellsignaling enzymes. JNK1 plays a central role in linking obesity andinsulin resistance. JNK2 and JNK3 may be involved in inflammatoryand neurological disorders, respectively. Small-molecule JNK inhibitorscould be valuable tools to study the therapeutic benefits of inhibitingthese enzymes and as leads for potential drugs targeting JNKs. In thisreport, we disclose a series of potent and highly selective JNK inhibitorswith good pharmacokinetic profiles.