| Literature DB >> 18364256 |
Stephen T Wrobleski1, Shuqun Lin, John Hynes, Hong Wu, Sidney Pitt, Ding Ren Shen, Rosemary Zhang, Kathleen M Gillooly, David J Shuster, Kim W McIntyre, Arthur M Doweyko, Kevin F Kish, Jeffrey A Tredup, Gerald J Duke, John S Sack, Murray McKinnon, John Dodd, Joel C Barrish, Gary L Schieven, Katerina Leftheris.
Abstract
A novel series of compounds based on the pyrrolo[2,1-f][1,2,4]triazine ring system have been identified as potent p38 alpha 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 p38 alpha enzyme.Entities:
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Year: 2008 PMID： 18364256 DOI： 10.1016/j.bmcl.2008.02.067
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823