Abstract
Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstream ERK phosphorylation in LOX tumors from mouse xenograft studies.
MeSH terms
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Animals
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Cell Line, Tumor
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Chemistry, Pharmaceutical / methods*
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Crystallography, X-Ray / methods
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Drug Design
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Humans
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Inhibitory Concentration 50
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Mice
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Models, Chemical
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Neoplasm Transplantation
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Phosphorylation
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / pharmacology*
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Proto-Oncogene Proteins B-raf / antagonists & inhibitors*
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Proto-Oncogene Proteins B-raf / chemistry*
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Pyrazoles / chemistry*
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raf Kinases / antagonists & inhibitors*
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raf Kinases / chemistry*
Substances
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Protein Kinase Inhibitors
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Pyrazoles
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Proto-Oncogene Proteins B-raf
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raf Kinases