In 2017,Cui, Jing; Peng, Xia; Gao, Dingding; Dai, Yang; Ai, Jing; Li, Yingxia published 《Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.HPLC of Formula: 105942-08-3 The information in the text is summarized as follows:
Fibroblast growth factor receptor (FGFR) is a potential target for cancer therapy because of its critical role in promoting cancer formation and progression. In a continuing effort to improve the cellular activity of hit compound 4-(4-ethylpiperazin-1-yl)-N-[6-(2-fluoro-3-methoxyphenyl)-1H-indazol-3-yl]benzamide bearing an indazole scaffold, which was previously discovered, several compounds harnessing fluorine substituents I [R1 = H, F; R2 = H, F; R3 = H, F; R4 = H, F; R5 = H, F; R6 = H, F; X = [2-(dimethylamino)ethyl](methyl)aminyl, (3R,5S)-3,5-dimethylpiperazin-1-yl, 4-methyl-1,4-diazepan-1-yl, etc.] were designed, synthesized and biol. evaluated. Besides, the region extended out to the ATP binding pocket toward solvent was also explored. Among them, compound I [R1 = R2 = R3 = R4 = R5 = H; R6 = F; X = 4-ethylpiperazin-1-yl] containing 2,6-difluoro-3-methoxyphenyl residue exhibited the most potent activities (FGFR1: less than 4.1 nM, FGFR2: 2.0 ± 0.8 nM). More importantly, compound I [R1 = R2 = R3 = R4 = R5 = H; R6 = F; X = 4-ethylpiperazin-1-yl] showed an improved antiproliferative effect against KG1 cell lines and SNU16 cell lines with IC50 values of 25.3 ± 4.6 nM and 77.4 ± 6.2 nM resp. In the part of experimental materials, we found many familiar compounds, such as 4-Bromo-2-fluorobenzonitrile(cas: 105942-08-3HPLC of Formula: 105942-08-3)
4-Bromo-2-fluorobenzonitrile(cas:105942-08-3) is used as a reagent in the synthesis of picolinamide derivatives as a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors.HPLC of Formula: 105942-08-3 4-Bromo-2-fluorobenzonitrile is also used in the preparation of fluorinated CB2 receptor agonists for PET imaging.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts