Mo, Cheng; Zhang, Zhang; Li, Yupeng; Huang, Minhao; Zou, Jian; Luo, Jinfeng; Tu, Zheng-Chao; Xu, Yong; Ren, Xiaomei; Ding, Ke; Lu, Xiaoyun published the artcile< Design and Optimization of 3'-(Imidazo[1,2-a]pyrazin-3-yl)-[1,1'-biphenyl]-3-carboxamides as Selective DDR1 Inhibitors>, Application In Synthesis of 51605-97-1, the main research area is imidazo pyrazinyl carboxamide derivative preparation DDR1 inhibitor cancer.
DDR1 is considered as a promising target for cancer therapy, and selective inhibitors against DDR1 over other kinases may be considered as promising therapeutic agents. Herein, we have identified a series of 3′-(imidazo[1,2-a]pyrazin-3-yl)-[1,1′-biphenyl]-3-carboxamides as novel selective DDR1 inhibitors. Among these, compound 8v potently inhibited DDR1 with an IC50 of 23.8 nM, while it showed less inhibitory activity against DDR2 (IC50 = 1740 nM) and negligible activities against Bcr-Abl (IC50 > 10μM) and c-Kit (IC50 > 10μM). 8v also exhibited excellent selectivity in a KINOMEscan screening platform with 468 kinases. This compound dose-dependently suppressed NSCLC cell tumorigenicity, migration, and invasion. Collectively, these studies support its potential application for treatment of NSCLC.
ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 51605-97-1 belongs to class bromides-buliding-blocks, and the molecular formula is C9H12BrN, Application In Synthesis of 51605-97-1.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary