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

Bioorg Med Chem Lett 2006 Jan 19;16(1):108-12. Epub 2005 Oct 19.

Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.

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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http://dx.doi.org/10.1016/j.bmcl.2005.09.035DOI Listing
January 2006

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