Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk)

作者：Moriarty Kevin J; Takahashi Hidenori^*; Pullen Steven S; Khine Hnin Hnin; Sallati Rosemarie H; Raymond Ernest L; Woska Joseph R Jr; Jeanfavre Deborah D; Roth Gregory P; Winters Michael P; Qiao Lei; Ryan Declan; DesJarlais Renee; Robinson Darius; Wilson Matthew; Bobko Mark; Cook Brian N; Lo Ho Yin; Nemoto Peter A; Kashem Mohammed A; Wolak John P; White Andre; Magolda Ronald L; Tomczuk Bruce

来源：Bioorganic & Medicinal Chemistry Letters, 2008, 18(20): 5545-5549.

DOI：10.1016/j.bmcl.2008.09.015

• SAR
• Itk
• inhibitor
• benzimidazole

A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. In this report, we discuss the structure-activity relationship (SAR), selectivity, and cell-based activity for the series. We also discuss the SAR associated with an X-ray structure of one of the small-molecule inhibitors bound to ITK.

• 出版日期2008-10-15
• 单位河北医科大学