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. 2008 Oct 15;18(20):5541-4.
doi: 10.1016/j.bmcl.2008.09.016. Epub 2008 Sep 7.

5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk)

Michael P Winters  1 , Darius J Robinson, Hnin Hnin Khine, Steven S Pullen, Joseph R Woska Jr, Ernest L Raymond, Rosemarie Sellati, Charles L Cywin, Roger J Snow, Mohammed A Kashem, John P Wolak, Josephine King, Paul V Kaplita, Lisa H Liu, Thomas M Farrell, Renee DesJarlais, Gregory P Roth, Hidenori Takahashi, Kevin J Moriarty
Affiliations

5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk)

Michael P Winters et al. Bioorg Med Chem Lett. .

Abstract

A series of novel 5-aminomethyl-1H-benzimidazole based inhibitors of Itk were prepared. Structure-activity relationships, selectivity and cell activity are reported for this series. Compound 2, a potent and selective antagonist of Itk, inhibited anti-CD3 antibody induced IL-2 production in vivo in mice.

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