Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.

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.

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http://dx.doi.org/10.1016/j.bmcl.2009.10.138DOI Listing
February 2010

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