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.
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.,Velcicky J, Feifel R, Hawtin S, Heng R, Huppertz C, Koch G, Kroemer M, Moebitz H, Revesz L, Scheufler C, Schlapbach A Bioorg Med Chem Lett. 2010 Feb 1;20(3):1293-7. Epub 2009 Nov 3. PMID:20060294
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