Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3- b ]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats

Journal of Medicinal Chemistry

Volumn 56, Issue 17, 2013, Pages 6651-6665

  Cui, J Jean ^a   Shen, Hong ^a   Tran Dubé, Michelle ^a   Nambu, Mitchell ^a   McTigue, Michele ^a   Grodsky, Neil ^a   Ryan, Kevin ^a   Yamazaki, Shinji ^a   Aguirre, Shirley ^a   Parker, Max ^a   Li, Qiuhua ^a   Zou, Helen ^a   Christensen, James ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [3 [1 (QUINOLIN 6 YL)ETHYL][1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 YL]BENZONITRILE; 2 [4 [1 [1 (QUINOLIN 6 YL)ETHYL] 1H [1,2,3]TRIAZOLO[4,5 B]PYRAZIN 6 YL] 1H PYRAZOL 1 YL]ETHANOL; 3 (QUINOLIN 6 YLMETHYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 AMINE; 3 [(1H PYRROLO[2,3 B]PYRIDIN 3 YL)METHYL] 6 (1 METHYL 1H PYRAZOL 4 YL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZINE; 3 [1 (1H PYRROLO[2,3 B]PYRIDIN 3 YL)ETHYL] 6 (1 METHYL 1H PYRAZOL 4 YL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZINE; 3 [3 [1 (QUINOLIN 6 YL)ETHYL][1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 YL]BENZONITRILE; 3 [3 [QUINOLIN 6 YLMETHYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 YL]BENZONITRILE; 4 [3 (QUINOLIN 6 YLMETHYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 YL]BENZONITRILE; 4 [3 [1 (1H PYRROLO[2,3 B]PYRIDIN 3 YL]ETHYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 YL)BENZONITRILE; 4 [3 [1 (QUINOLIN 6 YL)ETHYL][1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 YL]BENZONITRILE; 6 [1 [6 (1 METHYL 1H PYRAZOL 4 YL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]ETHYL]QUINOLINE; 6 [1 [6 (1 METHYL 1H PYRAZOL 4 YL] 1H [1,2,3]TRIAZOLO[4,5 B]PYRAZIN 1 YL]ETHYL]QUINOLINE; 6 [1 [6 (2,3 DIHYDROBENZO[B][1,4]DIOXIN 6 YL][1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]ETHYL]QUINOLINE; 6 [1 [6 (3 FLUORO 4 METHOXYPHENYL)[1,2,4]TRIAZOLO[4,3 B]PYRIAZIN 3 YL]ETHYL]QUINOLINE; 6 [1 [6 (3 METHYLPHENYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]ETHYL]QUINOLINE; 6 [1 [6 (3,4 DIFLUOROPHENYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]ETHYL]QUINOLINE; 6 [1 [6 (4 ETHANESULFONYLPHENYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]ETHYL]QUINOLINE; 6 [1 [6 (4 METHANESULFONYLPHENYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]ETHYL]QUINOLINE; 6 [1 [6 (4 METHOXY 3 METHYLPHENYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]ETHYL]QUINOLINE; 6 [[6 (1 METHYL 1H PYRAZOL 4 YL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]METHYL]QUINOLINE; 6 [[6 (3,4 DIFLUOROPHENYL)[1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 3 YL]METHYL]QUINOLINE; ANTINEOPLASTIC AGENT; N METHYL 4 [3 [1 (QUINOLIN 6 YL)ETHYL][1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 YL]BENZAMIDE; N,N DIMETHYL 5 [3 [1 (QUINOLIN 6 YL)ETHYL][1,2,4]TRIAZOLO[4,3 B]PYRIDAZIN 6 YL]PYRIDIN 2 AMINE; PF 04217903; PF 04254644; PHOSPHODIESTERASE INHIBITOR; PROTEIN TYROSINE KINASE INHIBITOR; SCATTER FACTOR RECEPTOR; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; BINDING ASSAY; CANCER INHIBITION; CONTROLLED STUDY; DISTRIBUTION VOLUME; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME INHIBITION; FEMALE; HEART MUSCLE; HEART MUSCLE CONTRACTILITY; HEART OUTPUT; HEART RATE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IN VIVO STUDY; MOUSE; MUSCLE ATROPHY; NONHUMAN; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT;

ANIMALS; CARDIOMYOPATHIES; FEMALE; HUMANS; MICE; MICE, NUDE; MODELS, MOLECULAR; PHOSPHODIESTERASE INHIBITORS; PROTEIN KINASE INHIBITORS; QUINOLINES; RATS; RECEPTOR PROTEIN-TYROSINE KINASES;

EID: 84884265760     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400926x     Document Type: Article

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