Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).
Bioorg Med Chem Lett
; 18(20): 5545-9, 2008 Oct 15.
Article
in En
| MEDLINE
| ID: mdl-18819799
ABSTRACT
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Benzimidazoles
/
Protein-Tyrosine Kinases
/
Microsomes, Liver
/
Carboxylic Acids
/
Chemistry, Pharmaceutical
/
Enzyme Inhibitors
/
Amides
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2008
Document type:
Article
Affiliation country:
Estados Unidos