Bioorg Med Chem Lett 2010 Feb 3;20(3):1293-7. Epub 2009 Nov 3.
Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
New, selective 3-aminopyrazole based MK2-inhibitors were discovered by scaffold hopping strategy. The new derivatives proved to inhibit intracellular phosphorylation of hsp27 as well as LPS-induced TNFalpha release in cells. In addition, selected derivative 14e also inhibited LPS-induced TNFalpha release in vivo.