通过支架跳跃策略发现的新型 3-氨基吡唑 MK-2 抑制剂。
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
机构信息
Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1293-7. doi: 10.1016/j.bmcl.2009.10.138. Epub 2009 Nov 3.
PMID:20060294
Abstract
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.
摘要
通过基于支架跃迁策略，发现了新型、选择性的 3-氨基吡唑基 MK2 抑制剂。新的衍生物被证明能够抑制细胞内 hsp27 的磷酸化以及 LPS 诱导的 TNFalpha 的释放。此外，所选衍生物 14e 还能抑制 LPS 诱导的 TNFalpha 在体内的释放。
Zotero 插件