Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 3, 2009, Pages 1026-1029

  Lyne, Paul D ^a   Aquila, Brian ^a   Cook, Donald J ^a   Dakin, Les A ^a   Ezhuthachan, Jay ^a   Ioannidis, Stephanos ^a   Pontz, Timothy ^a   Su, Mei ^a   Ye, Qing ^a   Zheng, Xiaolan ^a   Block, Michael H ^a   Cowen, Scott ^a   Deegan, Tracy L ^a   Lee, John W ^a   Scott, David A ^a   Custeau, Dominique ^a   Drew, Lisa ^a   Poondru, Srinivasu ^a   Shen, Minhui ^a   Wu, Allan ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

Amidoheteroaryl; B Raf; V600E

Indexed keywords

B RAF KINASE; B RAF KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE; PHOSPHOTRANSFERASE INHIBITOR; RAS PROTEIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL ASSAY; CONTROLLED STUDY; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME ASSAY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; MOUSE; MUTANT; NONHUMAN; PROTEIN DOMAIN; RAT; SIGNAL TRANSDUCTION; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; TUMOR MODEL;

ADMINISTRATION, ORAL; ANIMALS; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; MICE; MODELS, CHEMICAL; MUTATION; PROTO-ONCOGENE PROTEINS B-RAF; RAF KINASES; RAS PROTEINS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

MUS; RODENTIA;

EID: 58849123651     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.10.053     Document Type: Article

References (18)

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13. 50s calculated.
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