Schlapbach, Achim, Feifel, Roland, Hawtin, Stuart, Heng, Richard, Koch, Guido, Moebitz, Henrik, Revesz, Laszlo, Scheufler, Clemens, Velcicky, Juraj, Waelchli, Rudolf and Huppertz, Christine (2008) Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity. Bioorganic & Medicinal Chemistry Letters, 18 (23). pp. 6142-6146. ISSN 1464-3405

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.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez...
Additional Information:	author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords:	MK2; MAPKAPK-2; TNFa inhibition; Inflammation; Rheumatoid arthritis
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez...
Date Deposited:	14 Dec 2009 13:48
Last Modified:	31 Jan 2013 00:55
URI:	https://oak.novartis.com/id/eprint/1378