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

Bioorganic & medicinal chemistry letters 2009 Nov 3; In press

Link to PubMed abstract

Velcicky J, Feifel R, Hawtin S, Heng R, Huppertz C, Koch G, Kroemer M, Moebitz H, Revesz L, Scheufler C, Schlapbach A

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.

Keywords: MK-2