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

Schlapbach, Achim and Feifel, Roland and Hawtin, Stuart and Heng, Richard and Koch, Guido and Moebitz, Henrik and Revesz, Laszlo and Scheufler, Clemens and Velcicky, Juraj and 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
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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
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Date Deposited: 14 Dec 2009 13:48
Last Modified: 31 Jan 2013 00:55
URI: https://oak.novartis.com/id/eprint/1378

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