1392430-07-7Relevant articles and documents
Discovery of a highly specific and potent pan-RAF inhibitor
Hong, Sung Pyo,Lee, Younho,Choi, Nam Song,Nam, Ky-Youb,Ahn, Soon Kil
, p. 1632 - 1637 (2016)
We describe the structure-based design and synthesis of N-(2,6-difluorophenyl)-3-(9H-purin-6-yl)pyridine-2-amine derivatives as a selective pan-RAF kinase inhibitor. The synthesized compounds showed highly potent and specific inhibition of the BRAFV600E mutant cell line. Among them, N-(3-((3-(9H-purin-6-yl) pyridine-2-yl)amino)-2,4-difluorophenyl)furan-3-sulfonamide (4b) exhibited the most potent inhibitory activities against protein kinase enzymes BRAFV600E, BRAFWT, and CRAF (IC50 of 2, 2, and 1 nM, respectively) and a mutant cell line bearing a BRAFV600E mutation, A375P (GI50 of 7 nM).
Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors
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Page/Page column 27, (2013/02/27)
The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A, X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.