1227912-19-7Relevant articles and documents
Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors
Cui, Jing,Peng, Xia,Gao, Dingding,Dai, Yang,Ai, Jing,Li, Yingxia
supporting information, p. 3782 - 3786 (2017/07/27)
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 7r bearing an indazole scaffold, which was previously discovered by our group, several compounds harnessing fluorine substituents were designed, synthesized and biological evaluated. Besides, the region extended out to the ATP binding pocket toward solvent was also explored. Among them, compound 2a 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 2a 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 respectively.
N-ALKYLATED INDOLE AND INDAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
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Page/Page column 50, (2014/03/22)
The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.