• Title of article

    Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase

  • Author/Authors

    Bernard Barlaam، نويسنده , , David G. Acton، نويسنده , , Peter Ballard، نويسنده , , Robert H. Bradbury، نويسنده , , Darren Cross، نويسنده , , Richard Ducray، نويسنده , , Hervé Germain، نويسنده , , Kevin Hudson، نويسنده , , Teresa Klinowska، نويسنده , , Françoise Magnien، نويسنده , , Donald J. Ogilvie، نويسنده , , Annie Olivier، نويسنده , , Helen S. Ross، نويسنده , , Robin Smith، نويسنده , , Cath B. Trigwell، نويسنده , , Michel Vautier، نويسنده , , Lindsay Wright، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2008
  • Pages
    5
  • From page
    1799
  • To page
    1803
  • Abstract
    We have identified a new series of C-5 substituted indazolylaminoquinazolines as potent erbB2 kinase inhibitors. The lead compound 22 showed excellent in vitro potency, good physical properties, acceptable oral pharmacokinetics in rat and dog, and low human in vitro clearance. It showed at least equivalent activity dose for dose compared to lapatinib in various erbB2- or EGFR-driven xenograft models after chronic oral administration.
  • Keywords
    indazole , erbB2 kinase inhibitor , C-5 substitution , Quinazoline
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2008
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    799249

    • Link To Document
    https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=799249