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

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

  • Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. doi: 10.1016/j.bmcl.2005.09.035.
Rudolf Waelchli 1,  Birgit Bollbuck,  Christian Bruns,  Thomas Buhl,  Jörg Eder,  Roland Feifel,  Rene Hersperger,  Philipp Janser,  Laszlo Revesz,  Hans-Günter Zerwes,  Achim Schlapbach
Affiliations

Affiliation

  • 1 Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland. rudolf.waelchli@novartis.com
PMID: 16236504 DOI: 10.1016/j.bmcl.2005.09.035
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 IC(50) values of 40 and 25 nM, respectively. Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine release.

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