847608-28-0Relevant articles and documents
Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1h)-ones
Wallace, Eli M.,Lyssikatos, Joseph,Blake, James F.,Seo, Jeongbeob,Yang, Hong Woon,Yeh, Tammie C.,Perrier, Michele,Jarski, Heidi,Marsh, Vivienne,Poch, Gregory,Livingston, Michelle Goyette,Otten, Jennifer,Hingorani, Gary,Woessner, Rich,Lee, Patrice,Winkler, James,Koch, Kevin
, p. 441 - 444 (2007/10/03)
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.
Heterocyclic inhibitors of MEK and methods of use thereof
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, (2008/06/13)
Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.