1092486-06-0Relevant articles and documents
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
, p. 6218 - 6221 (2008)
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.