658700-11-9Relevant academic research and scientific papers
Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design
Cook, Brian N.,Bentzien, J?rg,White, Andre,Nemoto, Peter A.,Wang, Ji,Man, Chuk C.,Soleymanzadeh, Fariba,Khine, Hnin Hnin,Kashem, Mohammed A.,Kugler Jr., Stanley Z.,Wolak, John P.,Roth, Gregory P.,De Lombaert, Stéphane,Pullen, Steven S.,Takahashi, Hidenori
scheme or table, p. 773 - 777 (2009/08/15)
Interleukin-2 inducible T-cell kinase (ITK) is a member of the Tec kinase family and is involved with T-cell activation and proliferation. Due to its critical role in acting as a modulator of T-cells, ITK inhibitors could provide a novel route to anti-inf
2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket
Lo, Ho Yin,Bentzien, Joerg,Fleck, Roman W.,Pullen, Steven S.,Khine, Hnin Hnin,Woska Jr., Joseph R.,Kugler, Stanley Z.,Kashem, Mohammed A.,Takahashi, Hidenori
scheme or table, p. 6218 - 6221 (2009/07/18)
Based on the information from molecular modeling and X-ray crystal structures, the kinase specificity pocket of ITK could be occupied upon extension of the right-hand-side of the 2-benzimidazole core of the inhibitors. 2-Aminobenzimidazoles with a trans-stilbene-like extension were designed and synthesized as novel ITK antagonists. Significant improvement on binding affinity and cellular activity were obtained through the trans-stilbene-like antagonists. Several compounds showed inhibitory activity in an IL-2 functional assay.
Itk kinase inhibitors: Initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead
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
scheme or table, p. 5537 - 5540 (2009/06/30)
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 a
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.
THIOPHENE -2- CARBOXYLIC ACID - (1H - BENZIMIDAZOL - 2 YL) - AMIDE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE TEC KINASE ITK (INTERLEUKIN -2- INDUCIBLE T CELL KINASE) FOR THE TREATMENT OF INFLAMMATION, IMMUNOLOGICAL AND ALLERGIC DISORDERS
-
Page/Page column 129-131, (2010/02/13)
Disclosed are compounds of formula (I): wherein Ar1, Ar2, R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for
SUBSTITUTED BENZIMIDAZOLE COMPOUNDS
-
Page 155, (2008/06/13)
Disclosed are substituted benzimidazole compounds of formula (I) wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and the pharmaceutical compositions comprising these compounds.
