103977-79-3Relevant articles and documents
GCN2 MODULATOR COMPOUNDS
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, (2021/08/27)
The disclosures herein relate to novel compounds of Formula (1): or a salt thereof, wherein X, Y, R1, R2, R3, R4 and R5 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with General Control Nondepressible 2 (GCN2).
Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors
Chang, Yu,Lu, Xiaoyun,Shibu, Marthandam Asokan,Dai, Yi-Bo,Luo, Jinfeng,Zhang, Yan,Li, Yingjun,Zhao, Peng,Zhang, Zhang,Xu, Yong,Tu, Zheng-Chao,Zhang, Qing-Wen,Yun, Cai-Hong,Huang, Chih-Yang,Ding, Ke
, p. 5927 - 5932 (2017/07/22)
A series of N-(3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides were designed as the first class of highly selective ZAK inhibitors. The representative compound 3h strongly inhibits the kinase activity of ZAK with an IC50 of 3.3 n
N-(3-ethynyl-2,4-difluorophenyl)sulfonamide derivatives as selective Raf inhibitors
Li, Yingjun,Cheng, Huimin,Zhang, Zhang,Zhuang, Xiaoxi,Luo, Jinfeng,Long, Huoyou,Zhou, Yang,Xu, Yong,Taghipouran, Rana,Li, Dan,Patterson, Adam,Smaill, Jeff,Tu, Zhengchao,Wu, Donghai,Ren, Xiaomei,Ding, Ke
, p. 543 - 547 (2015/05/27)
A series of N-(3-ethynyl-2,4-difluorophenyl)sulfonamides were identified as new selective Raf inhibitors. The compounds potently inhibit B-RafV600E with low nanomolar IC50 values and exhibit excellent target specificity in a selectivity profiling investigation against 468 kinases. They strongly suppress proliferation of a panel of human cancer cell lines and patient-derived melanoma cells with B-RafV600E mutation while being significantly less potent to the cells with B-RafWT. The compounds also display favorable pharmacokinetic properties with a preferred example (3s) demonstrating significant in vivo antitumor efficacy in a xenograft mouse model of B-RafV600E mutated Colo205 human colorectal cancer cells, supporting it as a promising lead compound for further anticancer drug discovery.