• Title of article

    Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK

  • Author/Authors

    Rudolf Waelchli، نويسنده , , Birgit Bollbuck، نويسنده , , Christian Bruns، نويسنده , , Thomas Buhl، نويسنده , , J?rg Eder، نويسنده , , Roland Feifel، نويسنده , , Rene Hersperger، نويسنده , , Philipp Janser، نويسنده , , Laszlo Revesz، نويسنده , , Hans-Günter Zerwes، نويسنده , , Achim Schlapbach، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2006
  • Pages
    5
  • From page
    108
  • To page
    112
  • Abstract
    The design, synthesis, and the biological evaluation of 2-benzamido-pyrimidines as novel IKK inhibitors are described. By optimization of the lead compound 3, compounds 16 and 24 are identified as good inhibitors of IKK2 with IC50 values of 40 and 25 nM, respectively. Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine release.
  • Keywords
    IKK2 , IKK inhibitors , In vivo activity , 2-Benzamido-pyrimidines
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2006
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    796324