Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK
R Waelchli, B Bollbuck, C Bruns, T Buhl, J Eder… - Bioorganic & medicinal …, 2006 - Elsevier
R Waelchli, B Bollbuck, C Bruns, T Buhl, J Eder, R Feifel, R Hersperger, P Janser, L Revesz…
Bioorganic & medicinal chemistry letters, 2006•ElsevierThe 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 25nM, respectively.
Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine
release.
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 25nM, respectively.
Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine
release.
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 25nM, respectively. Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine release.
Elsevier