Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors was written by Fan, Jun;Dai, Yang;Shao, Jingwei;Peng, Xia;Wang, Chen;Cao, Sufen;Zhao, Bin;Ai, Jing;Geng, Meiyu;Duan, Wenhu. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2016.Name: Methyl 2-bromo-4-fluorobenzoate This article mentions the following:
Fibroblast growth factor receptors (FGFRs) are important oncol. targets due to the dysregulation of this signaling pathway in a wide variety of human cancers. The authors identified a series of pyrazolylaminoquinazoline derivatives as potent FGFR inhibitors with low nanomolar potency. The representative compound I strongly inhibited FGFR1-3 kinase activity and suppressed FGFR signaling transduction in FGFR-addicted cancer cells; FGFRs-driven cell proliferation was also strongly inhibited regardless of mechanistic complexity implicated in FGFR activation, which further confirmed that I was a potent pan-FGFR inhibitor. The flexibility of the structure offered the potential to preserve good affinity for mutant FGFR, which is important for developing TKIs with long-term efficacy. In the experiment, the researchers used many compounds, for example, Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9Name: Methyl 2-bromo-4-fluorobenzoate).
Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Name: Methyl 2-bromo-4-fluorobenzoate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary