Inhibitors of unactivated p38 MAP kinase

James Bullington, Dennis Argentieri, Kristin Averill, Demetrius Carter, Druie Cavender, Bohumila Fahmy, Xiaodong Fan, Daniel Hall, Geoffrey Heintzelman, Paul Jackson, Wai Ping Leung, Xun Li, Ping Ling, Gilbert Olini, Thomas Razler, Michael Reuman, Kenneth Rupert, Ronald Russell, John Siekierka, Scott WadsworthRussell Wolff, Bangping Xiang, Yue Mei Zhang

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

Inhibition of the p38 map kinase pathway has been shown to be beneficial in the treatment of inflammatory diseases. The first class of potent p38 kinase inhibitors was the pyridinylimidazole compounds from SKB. Since then several pyridinylimidazole-based compounds have been shown to inhibit activated p38 kinase in vitro and in vivo. We have developed a novel series of pyridinylimidazole-based compounds, which potently inhibit the p38 pathway by binding to unactivated p38 kinase and only weakly inhibiting activated p38 kinase activity in vitro.

Original languageEnglish
Pages (from-to)6102-6106
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number23
DOIs
StatePublished - 1 Dec 2006

Keywords

  • Kinase
  • Pyrrole
  • TNF
  • Toxicity
  • p38

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    Bullington, J., Argentieri, D., Averill, K., Carter, D., Cavender, D., Fahmy, B., Fan, X., Hall, D., Heintzelman, G., Jackson, P., Leung, W. P., Li, X., Ling, P., Olini, G., Razler, T., Reuman, M., Rupert, K., Russell, R., Siekierka, J., ... Zhang, Y. M. (2006). Inhibitors of unactivated p38 MAP kinase. Bioorganic and Medicinal Chemistry Letters, 16(23), 6102-6106. https://doi.org/10.1016/j.bmcl.2006.08.101