Vasbinder, Melissa M. published the artcileDiscovery and Optimization of a Novel Series of Potent Mutant B-RafV600E Selective Kinase Inhibitors, SDS of cas: 1008506-24-8, the publication is Journal of Medicinal Chemistry (2013), 56(5), 1996-2015, database is CAplus and MEDLINE.
B-Raf represents an attractive target for anticancer therapy, and the development of small mol. B-Raf inhibitors has delivered new therapies for metastatic melanoma patients. The authors have discovered a novel class of small mols. that inhibit mutant B-RafV600E kinase activity both in vitro and in vivo. Investigations into the structure-activity relationships of the series are presented along with efforts to improve upon the cellular potency, solubility, and pharmacokinetic profile. Compounds selectively inhibited B-RafV600E in vitro and showed preferential antiproliferative activity in mutant B-RafV600E cell lines and exhibited selectivity in a kinase panel against other kinases. Examples from this series inhibit growth of a B-RafV600E A375 xenograft in vivo at a well-tolerated dose. In addition, aminoquinazolines described herein were shown to display pERK elevation in nonmutant B-Raf cell lines in vitro.
Journal of Medicinal Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C11H8O3, SDS of cas: 1008506-24-8.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem