Literature DB >> 15955699

(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.

Mark J Bamford1, Nicholas Bailey, Susannah Davies, David K Dean, Leann Francis, Terence A Panchal, Christopher A Parr, Sanjeet Sehmi, Jon G Steadman, Andrew K Takle, James T Townsend, David M Wilson.   

Abstract

The novel imidazo[4,5-c]pyridine 1,2,5-oxadiazol-3-yl template affords an excellent start point for identification of inhibitors of a number of protein kinases. Here we report on its optimisation for mitogen and stress-activated protein kinase-1 (MSK-1) inhibitory activity, and selectivity over other kinases.

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Year:  2005        PMID: 15955699     DOI: 10.1016/j.bmcl.2005.05.020

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.

Authors:  Sylvain Couty; Isaac M Westwood; Andrew Kalusa; Celine Cano; Jon Travers; Kathy Boxall; Chiau Ling Chow; Sam Burns; Jessica Schmitt; Lisa Pickard; Caterina Barillari; P Craig McAndrew; Paul A Clarke; Spiros Linardopoulos; Roger J Griffin; G Wynne Aherne; Florence I Raynaud; Paul Workman; Keith Jones; Rob L M van Montfort
Journal:  Oncotarget       Date:  2013-10

2.  Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1.

Authors:  Adrian Hall; Jan Abendroth; Madison J Bolejack; Tom Ceska; Sylvie Dell'Aiera; Victoria Ellis; David Fox; Cyril François; Muigai M Muruthi; Camille Prével; Karine Poullennec; Sergei Romanov; Anne Valade; Alain Vanbellinghen; Jason Yano; Martine Geraerts
Journal:  ACS Med Chem Lett       Date:  2022-06-25       Impact factor: 4.632

3.  The Role of Mitogen-Activated Protein Kinase-Activated Protein Kinases (MAPKAPKs) in Inflammation.

Authors:  Ugo Moens; Sergiy Kostenko; Baldur Sveinbjørnsson
Journal:  Genes (Basel)       Date:  2013-03-26       Impact factor: 4.096

  3 in total

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