• Title of article

    2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCθ

  • Author/Authors

    L. Nathan Tumey، نويسنده , , Diane H. Boschelli، نويسنده , , Julie Lee، نويسنده , , Divya Chaudhary، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2008
  • Pages
    4
  • From page
    4420
  • To page
    4423
  • Abstract
    A series of 2-alkenyl thieno[2,3-b]pyridine inhibitors of PKCθ were synthesized as potential inflammatory modulators. This series led to the discovery of 2-alkenyl amides, which are exceptionally potent and selective inhibitors of PKCθ. Compound 8 has an IC50 of 3.8 nM against PKCθ and shows excellent selectivity over a variety of PKC isoforms.
  • Keywords
    nitrile , kinase , PKC? , PKC , Cyano , T cell , inflammation , Indole , thienopyridine , PKC?
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2008
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    799798