Article
Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold.
Journal of medicinal chemistry - 12 Jun 2008
Niculescu-Duvaz Ion, Roman Esteban, Whittaker Steven R, Friedlos Frank, Kirk Ruth, Scanlon Ian J, Davies Lawrence C, Niculescu-Duvaz Dan, Marais Richard, Springer Caroline J
Abstract excerpt
BRAF, a serine/threonine kinase, plays a key role in the development of certain types of cancer, particularly melanoma. 2-(3,4,5-Trimethoxyphenylamino)-6-(3-acetamidophenyl)-pyrazine, 1, was identified as a low micromolar (IC 50 = 3.5 microM) BRAF inhibitor from a high-throughput screen of a library of 23000 compounds. This compound was chosen as the starting point of a program aimed at developing inhibitors of...
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