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; Russell Wolff; Bangping Xiang; Yue Mei Zhang

doi:10.1016/j.bmcl.2006.08.101

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

Chemistry and Biochemistry

Research output: Contribution to journal › Article › peer-review

13 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 language	English
Pages (from-to)	6102-6106
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2006.08.101
State	Published - 1 Dec 2006

Keywords

Kinase
Pyrrole
TNF
Toxicity
p38

Access to Document

10.1016/j.bmcl.2006.08.101

Cite this

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

@article{6a3aa50af77841b9b8d4773ccf0a3e6c,

title = "Inhibitors of unactivated p38 MAP kinase",

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.",

keywords = "Kinase, Pyrrole, TNF, Toxicity, p38",

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

year = "2006",

month = dec,

day = "1",

doi = "10.1016/j.bmcl.2006.08.101",

language = "English",

volume = "16",

pages = "6102--6106",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "23",

}

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

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.

AB - 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.

KW - Kinase

KW - Pyrrole

KW - TNF

KW - Toxicity

KW - p38

UR - http://www.scopus.com/inward/record.url?scp=33750526440&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2006.08.101

DO - 10.1016/j.bmcl.2006.08.101

M3 - Article

C2 - 16971122

AN - SCOPUS:33750526440

SN - 0960-894X

VL - 16

SP - 6102

EP - 6106

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 23

ER -

Inhibitors of unactivated p38 MAP kinase

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this