Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl- piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase

Journal of Medicinal Chemistry

Volumn 54, Issue 20, 2011, Pages 7066-7083

  Guagnano, Vito ^a   Furet, Pascal ^a   Spanka, Carsten ^a   Bordas, Vincent ^a   Le Douget, Mickaël ^a   Stamm, Christelle ^a   Brueggen, Josef ^a   Jensen, Michael R ^a   Schnell, Christian ^a   Schmid, Herbert ^a   Wartmann, Markus ^a   Berghausen, Joerg ^a   Drueckes, Peter ^a   Zimmerlin, Alfred ^a   Bussiere, Dirksen ^c   Murray, Jeremy ^b   Graus Porta, Diana ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b GENENTECH INC   (United States)

^c NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (2,6 DICHLORO 3,5 DIMETHOXY PHENYL) 1 [6 [4 (4 ETHYLPIPERAZIN 1 YL)PHENYLAMINO]PYRIMIDIN 4 YL] 1 METHYLUREA; ANTINEOPLASTIC AGENT; FIBROBLAST GROWTH FACTOR RECEPTOR 1; FIBROBLAST GROWTH FACTOR RECEPTOR 2; FIBROBLAST GROWTH FACTOR RECEPTOR 3; NVP BGJ 398; PROTEIN TYROSINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIANGIOGENIC ACTIVITY; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BLADDER CANCER; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; FEMALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANGIOGENESIS INHIBITORS; ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; HUMANS; MICE; MICE, NUDE; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; PHENYLUREA COMPOUNDS; PYRIMIDINES; RATS; RATS, WISTAR; RECEPTOR PROTEIN-TYROSINE KINASES; RECEPTOR, FIBROBLAST GROWTH FACTOR, TYPE 3; RECEPTORS, FIBROBLAST GROWTH FACTOR; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS; URINARY BLADDER NEOPLASMS;

EID: 80054900437     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2006222     Document Type: Article

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