Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors

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• 作者：Jagabandhu Das ; Chunjian Liu ; Robert V. Moquin ; James Lin ; Joseph A. Furch ; Steven H. Spergel ; Kim W. McIntyre ; David J. Shuster ; Kathleen D. O’ ; Day ; Becky Penhallow et al.
• 关键词：Selective Itk inhibitors ; Thiazoles
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 May 2006
• 年：2006
• 卷：16
• 期：9
• 页码：2411-2415
• 全文大小：169 K

文摘

A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure–activity relationships (SARs), selectivity and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound 2 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo.