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 ,
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
