Title of article
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38α MAP kinase inhibitors
Author/Authors
Stephen T. Wrobleski، نويسنده , , Shuqun Lin، نويسنده , , John Hynes Jr.، نويسنده , , Hong Wu، نويسنده , , Sidney Pitt، نويسنده , , Ding Ren Shen، نويسنده , , Rosemary Zhang، نويسنده , , Kathleen M. Gillooly، نويسنده , , David J. Shuster، نويسنده , , Kim W. McIntyre، نويسنده , , Arthur M. Doweyko، نويسنده , , Kevin F. Kish، نويسنده , , Jeffrey A. Tredup، نويسنده , , Gerald J. Duke، نويسنده , , John S. Sack، نويسنده , , Murray McKinnon، نويسنده , , John Dodd، نويسنده , , Joel C. Barrish، نويسنده , , Gary L. Schieven، نويسنده , , Katerina Leftheris، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
2739
To page
2744
Abstract
A novel series of compounds based on the pyrrolo[2,1-f][1,2,4]triazine ring system have been identified as potent p38α MAP kinase inhibitors. The synthesis, structure–activity relationships (SAR), and in vivo activity of selected analogs from this class of inhibitors are reported. Additional studies based on X-ray co-crystallography have revealed that one of the potent inhibitors from this series binds to the DFG-out conformation of the p38α enzyme.
Keywords
P38 , kinase , inflammation , Pyrrolotriazines , TNF-? , IL-1
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799441
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