Novel thiazole derivatives incorporating phenyl sulphonyl moiety as potent BRAFV600E kinase inhibitors targeting melanoma

Abstract

Thiazole derivatives 7b and 13a were superior to dabrafenib against B-RAFV600E kinase and potently inhibited the growth of WM266.4 melanoma cells. Compound 7b suppressed the phosphorylation of downstream ERK1/2 from WM266.4 cells.

Design, and synthesis of selectively anticancer 4-cyanophenyl substituted thiazol-2-ylhydrazones

“…However, we note that very recently a related group of thiazoles were described that are potent kinase inhibitors. 40 It is possible that our own compounds operate similarly as preliminary experiments also showed ERK1/2 inhibition for 3f. In conclusion, these synthetically accessible molecules are worthy of further preclinical evaluation including further examination against broad-spectrum cancer phenotypes and elucidation of their mechanism of action.…”