Novel 3-Aminopyrazole Inhibitors Of Mk-2 Discovered By Scaffold Hopping Strategy

Juraj Velcicky,Roland Feifel,Stuart Hawtin,Richard Heng,Christine Huppertz,Guido Koch,Markus Kroemer,Henrik Moebitz,Laszlo Revesz,Clemens Scheufler,Achim Schlapbach

Bioorganic & medicinal chemistry letters（2010）

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摘要

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 TNF alpha release in cells. In addition, selected derivative 14e also inhibited LPS-induced TNF alpha release in vivo. (C) 2009 Elsevier Ltd. All rights reserved.

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关键词

MK2,TNF alpha-inhibition,3-Aminopyrazole,Scaffold hopping,Induced-fit,X-ray

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