Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).

doi:10.1021/jm801509w

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Article

Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).

Journal of medicinal chemistry - 23 Apr 2009

Niculescu-Duvaz Dan, Gaulon Catherine, Dijkstra Harmen P, Niculescu-Duvaz Ion, Zambon Alfonso, Ménard Delphine, Suijkerbuijk Bart M J M, Nourry Arnaud, Davies Lawrence, Manne Helen, Friedlos Frank, Ogilvie Lesley, Hedley Douglas, Whittaker Steven, Kirk Ruth, Gill Adrian, Taylor Richard D, Raynaud Florence I, Moreno-Farre Javier, Marais Richard, Springer Caroline J

Abstract excerpt

BRAF is a serine/threonine kinase that is mutated in a range of cancers, including 50-70% of melanomas, and has been validated as a therapeutic target. We have designed and synthesized mutant BRAF inhibitors containing pyridoimidazolone as a new hinge-binding scaffold. Compounds have been obtained which have low nanomolar potency for mutant BRAF (12 nM for compound 5i) and low micromolar cellular potency against...

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PMID: 19323560
DOI: 10.1021/jm801509w

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BRAF

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

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