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

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

Bioorganic & medicinal chemistry letters (2005-10-21)

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

PMID16236504

摘要

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 IC(50) values of 40 and 25 nM, respectively. Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine release.