Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5] cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met

Journal of Medicinal Chemistry

Volumn 56, Issue 6, 2013, Pages 2294-2310

  Northrup, Alan B ^a   Katcher, Matthew H ^a   Altman, Michael D ^a   Chenard, Melissa ^a   Daniels, Matthew H ^a   Deshmukh, Sujal V ^a   Falcone, Danielle ^a   Guerin, David J ^a   Hatch, Harold ^a   Li, Chaomin ^a   Lu, Wei ^a   Lutterbach, Bart ^a   Allison, Timothy J ^a   Patel, Sangita B ^a   Reilly, John F ^a   Reutershan, Michael ^a   Rickert, Keith W ^a   Rosenstein, Craig ^a   Soisson, Stephen M ^a   Szewczak, Alexander A ^a   Walker, Deborah ^a   Wilson, Kevin ^a   Young, Jonathan R ^a   Pan, Bo Sheng ^a   Dinsmore, Christopher J ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [3 (1 METHYL 1H PYRAZOL 4 YL) 5 OXO 5H BENZO[4,5]CYCLOHEPTA[1,2 B]PYRIDIN 7 YL] N (PYRIDIN 2 YLMETHYL)METHANESULFONAMIDE; CYTOCHROME P450 3A4; CYTOKINE RECEPTOR ANTAGONIST; MK 8033; PROTEIN KINASE INHIBITOR; SCATTER FACTOR RECEPTOR; SULFONAMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG POTENCY; ENZYME CONFORMATION; ENZYME INHIBITION; GENE MUTATION; HUMAN; HUMAN CELL; NONHUMAN; RAT; TUMOR GROWTH; TUMOR XENOGRAFT; X RAY CRYSTALLOGRAPHY;

ANIMALS; BENZOCYCLOHEPTENES; CELL LINE, TUMOR; DOGS; DRUG DISCOVERY; ENZYME ACTIVATION; FEMALE; HUMANS; MICE; MODELS, MOLECULAR; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-MET; RATS; RECEPTOR PROTEIN-TYROSINE KINASES; SUBSTRATE SPECIFICITY; SULFONAMIDES; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84875733618     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301619u     Document Type: Article

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