Itk kinase inhibitors: Initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead

作者：Moriarty Kevin J; Winters Michael; Qiao Lei; Ryan Declan; DesJarlis Renee; Robinson Darius; Cook Brian N; Kashem Mohammed A; Kaplita Paul V; Liu Lisa H; Farrell Thomas M; Khine Hnin Hnin; King Josephine; Pullen Steven S; Roth Gregory P; Magolda Ronald; Takahashi Hidenori^*

来源：Bioorganic & Medicinal Chemistry Letters, 2008, 18(20): 5537-5540.

DOI：10.1016/j.bmcl.2008.09.017

• SAR
• Itk inhibitor
• metabolic stability
• liver microsomes

Previously, we reported a series of novel benzimidazole based Itk inhibitors that exhibited excellent enzymatic potency and selectivity but low microsomal stability. Employing a structure based approach a new series of inhibitors with comparable potency and selectivity to the original series and with a potential for improved microsome stability was identified.

• 出版日期2008-10-15
• 单位河北医科大学