Literature DB >> 18823779

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

Michael P Winters1, Darius J Robinson, Hnin Hnin Khine, Steven S Pullen, Joseph R Woska, 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.   

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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Year:  2008        PMID: 18823779     DOI: 10.1016/j.bmcl.2008.09.016

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Imidoyl dichlorides as new reagents for the rapid formation of 2-aminobenzimidazoles and related azoles.

Authors:  Julie A Pollock; Sung Hoon Kim; John A Katzenellenbogen
Journal:  Tetrahedron Lett       Date:  2015-10-28       Impact factor: 2.415

2.  Copper-mediated amidation of heterocyclic and aromatic C-H bonds.

Authors:  Qiu Wang; Stuart L Schreiber
Journal:  Org Lett       Date:  2009-11-19       Impact factor: 6.005

  2 in total

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