Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf V600E kinase with favorable physicochemical and pharmacokinetic properties

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 2, 2012, Pages 1165-1168

  Ren, Li ^a   Laird, Ellen R ^a   Buckmelter, Alex J ^a   Dinkel, Victoria ^a   Gloor, Susan L ^a   Grina, Jonas ^a   Newhouse, Brad ^a   Rasor, Kevin ^a   Hastings, Gregg ^a   Gradl, Stefan N ^b   Rudolph, Joachim ^b  

^a ARRAY BIOPHARMA INC   (United States)

^b GENENTECH INC   (United States)

Author keywords

B Raf; Cancer; Drug discovery; Kinase

Indexed keywords

ADENOSINE TRIPHOSPHATE; B RAF KINASE; B RAF KINASE INHIBITOR; CYTOCHROME P450 3A4; PYRAZOLO[1,5 ALPHA]PYRIMIDINE; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CANCER INHIBITION; CELL STRAIN CACO 2; CRYSTAL STRUCTURE; DISTRIBUTION VOLUME; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; DRUG SOLUBILITY; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME INHIBITION; HYDROGEN BOND; HYDROPHOBICITY; IC 50; MICROSOME; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY;

ANIMALS; CHEMISTRY, PHYSICAL; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; MICE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTO-ONCOGENE PROTEINS B-RAF; PYRAZOLES; PYRIMIDINES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84855666466     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.092     Document Type: Article

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