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Bioorg Med Chem Lett. 2008 Dec 1;18(23):6142-6. doi: 10.1016/j.bmcl.2008.10.039. Epub 2008 Oct 11.

Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.

Author information

1
Novartis Institutes for BioMedical Research, global Discovery Chemistry, WSJ-88.508, CH-4002 Basel, Switzerland. achim.schlapbach@novartis.com

Abstract

Pyrrolo-pyrimidones of the general structure 1 were synthesized and evaluated for their potential as MK2 inhibitors. Potent derivatives were discovered which inhibit MK2 in the nanomolar range and show potent inhibition of cytokine release from LPS-stimulated monocytes. These derivatives were shown to inhibit phosphorylation of hsp27, a downstream target of MK2 and are modestly selective in a panel of 28 kinases.

PMID:
18945615
DOI:
10.1016/j.bmcl.2008.10.039
[Indexed for MEDLINE]

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