821791-44-0Relevant academic research and scientific papers
4-Anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase
Spicer, Julie A.,Rewcastle, Gordon W.,Kaufman, Michael D.,Black, Shannon L.,Plummer, Mark S.,Denny, William A.,Quin III, John,Shahripour, Aurash B.,Barrett, Stephen D.,Whitehead, Christopher E.,Milbank, Jared B. J.,Ohren, Jeffrey F.,Gowan, Richard C.,Omer, Charles,Camp, Heidi S.,Esmaeil, Nadia,Moore, Kelley,Sebolt-Leopold, Judith S.,Pryzbranowski, Sally,Merriman, Ronald L.,Ortwine, Daniel F.,Warmus, Joseph S.,Flamme, Cathlin M.,Pavlovsky, Alexander G.,Tecle, Haile
, p. 5090 - 5102 (2008/03/13)
A new series of MEK1 inhibitors, the 4-anilino-5-carboxamido-2-pyridones, were designed and synthesized using a combination of medicinal chemistry, computational chemistry, and structural elucidation. The effect of variation in the carboxamide side chain,
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.
5-SUBSTITUTED-4-`(SUBSTITUTED PHENYL)!AMINO!-2-PYRIDONE DEVIATIVES FOR USE AS MEK INHIBITORS
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Page 76, (2010/02/10)
The present invention relates to 5-substituted-4-(substituted) phenylamino-2-pyridone derivatives of formula (I), pharmaceutical compositions and methods of use thereof as MEK inhibitors. Formula (I) wherein W is formula (II), formula (III), formula (IV),
