| Autor: |
Wrobleski ST; Department of Immunology Chemistry, Bristol-Myers Squibb, Princeton, NJ 08543-4000, USA. stephen.wrobleski@bms.com, Lin S, Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Gillooly KM, Shuster DJ, McIntyre KW, Doweyko AM, Kish KF, Tredup JA, Duke GJ, Sack JS, McKinnon M, Dodd J, Barrish JC, Schieven GL, Leftheris K |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Apr 15; Vol. 18 (8), pp. 2739-44. Date of Electronic Publication: 2008 Mar 04. |
| DOI: |
10.1016/j.bmcl.2008.02.067 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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