Discovery of a new class of p38 kinase inhibitors

…, J Kingery-Wood, WJ Scott, RA Smith, M Bobko…

Index: Dumas, Jacques; Sibley, Robert; Riedl, Bernd; Monahan, Mary Katherine; Lee, Wendy; Lowinger, Timothy B.; Redman, Aniko M.; Johnson, Jeffrey S.; Kingery-Wood, Jill; Scott, William J.; Smith, Roger A.; Bobko, Mark; Schoenleber, Robert; Ranges, Gerald E.; Housley, Timothy J.; Bhargava, Ajay; Wilhelm, Scott M.; Shrikhande, Alka Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 18 p. 2047 - 2050

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Citation Number: 65

Abstract

The MAP kinase p38 has been implicated in cytokine signaling, and its inhibitors are potentially useful for the treatment of arthritis and osteoporosis. Novel small-molecule inhibitors of p38 kinase were derived from a combinatorial chemistry effort and exhibit activity in the nanomolar range. Very steep structure–activity relationships are observed within this class.