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

2009; Elsevier BV; Volume: 20; Issue: 3 Linguagem: Inglês

10.1016/j.bmcl.2009.10.138

1464-3405

Juraj Velcicky, Roland Feifel, Stuart Hawtin, Richard Heng, Christine Huppertz, Guido Koch, M. Kroemer, Henrik Moebitz, Láśzló Révész, Clemens Scheufler, Achim Schlapbach,

Cytokine Signaling Pathways and Interactions

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 TNFα release in cells. In addition, selected derivative 14e also inhibited LPS-induced TNFα release in vivo.