| Autor: |
Wallace EM; Array BioPharma, Boulder, Colorado 80301, USA. ewallace@arraybiopharma.com, Lyssikatos J, Blake JF, Seo J, Yang HW, Yeh TC, Perrier M, Jarski H, Marsh V, Poch G, Livingston MG, Otten J, Hingorani G, Woessner R, Lee P, Winkler J, Koch K |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2006 Jan 26; Vol. 49 (2), pp. 441-4. |
| DOI: |
10.1021/jm050834y |
| Abstrakt: |
The role of MEK 1,2 in cancer tumorgenesis has been clearly demonstrated preclinically, and two selective inhibitors are currently undergoing clinical evaluation to determine their role in the human disease. We have discovered 4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1H)-ones as a new class of ATP noncompetitive MEK inhibitors. These inhibitors exhibit excellent cellular potency and good pharmacokinetic properties and have demonstrated the ability to inhibit ERK phosphorylation in HT-29 tumors from mouse xenograft studies. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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