A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors

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• 作者：Tiansheng Wang ; Mark W. Ledeboer ; John P. Duffy ; Albert C. Pierce ; Harmon J. Zuccola ; Eric Block ; Dina Shlyakter ; James K. Hogan ; Youssef L. Bennani
• 关键词：Azaindole ; Deazapurine ; JAK2 ; Kinase ; Inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 January 2010
• 年：2010
• 卷：20
• 期：1
• 页码：153-156
• 全文大小：560 K

文摘

Pictet–Spengler condensation of aldehydes or alpha-keto-esters with 4-(2-anilinophenyl)-7-azaindole (11) or deazapurine (12) gave high yields of the 3,4-fused cyclic compounds. SAR studies, by varying the substituted benzaldehyde components, lead to the discovery of a series of potent JAK2 kinase inhibitors.