Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors |
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| Authors: | Wrobleski Stephen T Lin Shuqun Hynes John Wu Hong Pitt Sidney Shen Ding Ren Zhang Rosemary Gillooly Kathleen M Shuster David J McIntyre Kim W Doweyko Arthur M Kish Kevin F Tredup Jeffrey A Duke Gerald J Sack John S McKinnon Murray Dodd John Barrish Joel C Schieven Gary L Leftheris Katerina |
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| Institution: | Department of Immunology Chemistry, Bristol-Myers Squibb, Princeton, NJ 08543-4000, USA. stephen.wrobleski@bms.com |
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| Abstract: | A novel series of compounds based on the pyrrolo2,1-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. |
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