Niculescu-Duvaz, Dan published the artcilePotent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents, Quality Control of 1219130-56-9, the publication is Bioorganic & Medicinal Chemistry (2013), 21(5), 1284-1304, database is CAplus and MEDLINE.
The RAS-RAF-MEK-ERK pathway is hyperactivated in 30% of cancers. BRAF is a serine-threonine kinase, belonging to this pathway that is mutated with high frequency in melanoma and other cancers thus BRAF is an important therapeutic target in melanoma. We have designed inhibitors of BRAF based on 2,4,5-trisubstituted imidazoles with naphthyl and benzothiophene-4-substituents. Two compounds were discovered to be potent BRAF inhibitors: 1-(6-{2-[4-(2-dimethylamino-ethoxy)phenyl]-5-(pyridin-4-yl)-1H-imidazol-4-yl}benzo[b]thiophen-3-yl)-2,2,2-trifluoroethanol with BRAF IC50 = 190 nM and with cellular GI50 = 2100 nM, and 6-{2-[4-(2-dimethylamino-ethoxy)-phenyl]-5-pyridin-4-yl-3H-imidazol-4-yl}-naphthalen-1-ol with IC50 = 9 nM and GI50 = 220 nM.
Bioorganic & Medicinal Chemistry published new progress about 1219130-56-9. 1219130-56-9 belongs to isoquinoline, auxiliary class Isoquinoline,Boronic acid and ester,Amide,Boronic Acids,Boronate Esters, name is 6-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)isoquinolin-1(2H)-one, and the molecular formula is C15H18BNO3, Quality Control of 1219130-56-9.
Referemce:
https://en.wikipedia.org/wiki/Isoquinoline,
Isoquinoline | C9H7N – PubChem