Article
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.
Bioorganic & medicinal chemistry - 15 Sept 2010
Niculescu-Duvaz Dan, Niculescu-Duvaz Ion, Suijkerbuijk Bart M J M, Ménard Delphine, Zambon Alfonso, Nourry Arnaud, Davies Lawrence, Manne Helen A, Friedlos Frank, Ogilvie Lesley, Hedley Douglas, Takle Andrew K, Wilson David M, Pons Jean-Francois, Coulter Tom, Kirk Ruth, Cantarino Neus, Whittaker Steven, Marais Richard, Springer Caroline J
Abstract excerpt
V-RAF murine sarcoma viral oncogene homolog B1 (BRAF) is a serine/threonine-specific protein kinase that is mutated with high frequency in cutaneous melanoma, and many other cancers. Inhibition of mutant BRAF is an attractive therapeutic approach for the treatment of melanoma. A triarylimidazole BRAF inhibitor bearing a phenylpyrazole group...
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