658700-06-2Relevant academic research and scientific papers
Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk)
Moriarty, Kevin J.,Takahashi, Hidenori,Pullen, Steven S.,Khine, Hnin Hnin,Sallati, Rosemarie H.,Raymond, Ernest L.,Woska Jr., Joseph R.,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, André,Magolda, Ronald L.,Tomczuk, Bruce
scheme or table, p. 5545 - 5549 (2009/06/18)
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.
Hit-to-lead studies on benzimidazole inhibitors of ITK: Discovery of a novel class of kinase inhibitors
Snow, Roger J.,Abeywardane, Asitha,Campbell, Scot,Lord, John,Kashem, Mohammed A.,Khine, Hnin Hnin,King, Josephine,Kowalski, Jennifer A.,Pullen, Steven S.,Roma, Teresa,Roth, Gregory P.,Sarko, Christopher R.,Wilson, Noel S.,Winters, Michael P.,Wolak, John P.,Cywin, Charles L.
, p. 3660 - 3665 (2008/02/09)
Benzimidazole 1 was identified as a selective inhibitor of ITK by high throughput screening. Hit-to-lead studies defined the SAR at all three substituents. Reversing the amide linkage at C6 led to 16, with a fivefold improvement of potency. This enhanceme
