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 Wadsworth & 3 others Russell Wolff, Bangping Xiang, Yue Mei Zhang

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

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

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p38 Mitogen-Activated Protein Kinases
Phosphotransferases
MAP Kinase Signaling System
In Vitro Techniques

Keywords

  • Kinase
  • Pyrrole
  • TNF
  • Toxicity
  • p38

Cite this

Bullington, J., Argentieri, D., Averill, K., Carter, D., Cavender, D., Fahmy, B., ... 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
Bullington, James ; Argentieri, Dennis ; Averill, Kristin ; Carter, Demetrius ; Cavender, Druie ; Fahmy, Bohumila ; Fan, Xiaodong ; Hall, Daniel ; Heintzelman, Geoffrey ; Jackson, Paul ; Leung, Wai Ping ; Li, Xun ; Ling, Ping ; Olini, Gilbert ; Razler, Thomas ; Reuman, Michael ; Rupert, Kenneth ; Russell, Ronald ; Siekierka, John ; Wadsworth, Scott ; Wolff, Russell ; Xiang, Bangping ; Zhang, Yue Mei. / Inhibitors of unactivated p38 MAP kinase. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 23. pp. 6102-6106.
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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, WP, Li, X, Ling, P, Olini, G, Razler, T, Reuman, M, Rupert, K, Russell, R, Siekierka, J, Wadsworth, S, Wolff, R, Xiang, B & Zhang, YM 2006, 'Inhibitors of unactivated p38 MAP kinase', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 23, pp. 6102-6106. https://doi.org/10.1016/j.bmcl.2006.08.101

Inhibitors of unactivated p38 MAP kinase. / Bullington, James; Argentieri, Dennis; Averill, Kristin; Carter, Demetrius; Cavender, Druie; Fahmy, Bohumila; Fan, Xiaodong; Hall, Daniel; Heintzelman, Geoffrey; Jackson, Paul; Leung, Wai Ping; Li, Xun; Ling, Ping; Olini, Gilbert; Razler, Thomas; Reuman, Michael; Rupert, Kenneth; Russell, Ronald; Siekierka, John; Wadsworth, Scott; Wolff, Russell; Xiang, Bangping; Zhang, Yue Mei.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 23, 01.12.2006, p. 6102-6106.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Inhibitors of unactivated p38 MAP kinase

AU - Bullington, James

AU - Argentieri, Dennis

AU - Averill, Kristin

AU - Carter, Demetrius

AU - Cavender, Druie

AU - Fahmy, Bohumila

AU - Fan, Xiaodong

AU - Hall, Daniel

AU - Heintzelman, Geoffrey

AU - Jackson, Paul

AU - Leung, Wai Ping

AU - Li, Xun

AU - Ling, Ping

AU - Olini, Gilbert

AU - Razler, Thomas

AU - Reuman, Michael

AU - Rupert, Kenneth

AU - Russell, Ronald

AU - Siekierka, John

AU - Wadsworth, Scott

AU - Wolff, Russell

AU - Xiang, Bangping

AU - Zhang, Yue Mei

PY - 2006/12/1

Y1 - 2006/12/1

N2 - 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.

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KW - Pyrrole

KW - TNF

KW - Toxicity

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SP - 6102

EP - 6106

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 23

ER -

Bullington J, Argentieri D, Averill K, Carter D, Cavender D, Fahmy B et al. Inhibitors of unactivated p38 MAP kinase. Bioorganic and Medicinal Chemistry Letters. 2006 Dec 1;16(23):6102-6106. https://doi.org/10.1016/j.bmcl.2006.08.101