Literature DB >> 18835164

'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.

Antonio Garrido Montalban1, Erik Boman, Chau-Dung Chang, Susana Conde Ceide, Russell Dahl, David Dalesandro, Nancy G J Delaet, Eric Erb, Andrew Gibbs, Jeff Kahl, Linda Kessler, Jan Lundström, Stephen Miller, Hiroshi Nakanishi, Ed Roberts, Eddine Saiah, Robert Sullivan, Zhijun Wang, Christopher J Larson.   

Abstract

We have identified a second series of potent p38 inhibitors. As with our first generation series, these compounds are based on an alpha-ketoamide scaffold. The reversal of the ketoamide order, however, introduces more chemical flexibility and in addition results in improve potencies against p38.

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Year:  2008        PMID: 18835164     DOI: 10.1016/j.bmcl.2008.09.028

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


  1 in total

1.  A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.

Authors:  Sudharshan Eathiraj; Rocio Palma; Marscha Hirschi; Erika Volckova; Enkeleda Nakuci; Jennifer Castro; Chang-Rung Chen; Thomas C K Chan; Dennis S France; Mark A Ashwell
Journal:  J Biol Chem       Date:  2011-03-24       Impact factor: 5.157

  1 in total

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