Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors

Journal of Medicinal Chemistry

Volumn 53, Issue 15, 2010, Pages 5639-5655

  Zambon, Alfonso ^a   Ménard, Delphine ^a   Suijkerbuijk, Bart M J M ^a   Niculescu Duvaz, Ion ^a   Whittaker, Steven ^a   Niculescu Duvaz, Dan ^a   Nourry, Arnaud ^a   Davies, Lawrence ^a   Manne, Helen A ^a   Lopes, Filipa ^a   Preece, Natasha ^a   Hedley, Douglas ^a   Ogilvie, Lesley M ^a   Kirk, Ruth ^a   Marais, Richard ^a   Springer, Caroline J ^a  

^a IMPERIAL CANCER RESEARCH FUND   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

B RAF KINASE; B RAF KINASE INHIBITOR; IMIDAZO[4,5]PYRIDIN 2 ONE DERIVATIVE; IMIDAZOPYRIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTINEOPLASTIC ACTIVITY; ARTICLE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG HALF LIFE; DRUG SYNTHESIS; ENZYME INHIBITOR INTERACTION; FEMALE; HUMAN; HUMAN CELL; IC 50; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; REACTION OPTIMIZATION; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BENZENESULFONATES; BIOLOGICAL AVAILABILITY; CRYSTALLOGRAPHY, X-RAY; FEMALE; HUMANS; HYDROGEN BONDING; IMIDAZOLES; MICE; MICE, INBRED BALB C; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; PROTEIN BINDING; PROTO-ONCOGENE PROTEINS B-RAF; PYRAZINES; PYRIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSPLANTATION, HETEROLOGOUS;

EID: 77955355464     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100383b     Document Type: Article

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