In 2015,Jiang, Xiaolong; Liu, Hongyan; Song, Zilan; Peng, Xia; Ji, Yinchun; Yao, Qizheng; Geng, Meiyu; Ai, Jing; Zhang, Ao published 《Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d]isoxazole or 3-aminoindazole scaffold》.Bioorganic & Medicinal Chemistry published the findings.Category: pyrazoles-derivatives The information in the text is summarized as follows:
A series of 3-amino-benzo[d]isoxazole-/3-aminoindazole-based compounds were designed, synthesized and pharmacol. evaluated as tyrosine kinase c-Met inhibitors. The SAR study was conducted leading to identification of nine compounds with IC50s less than 10 nM against c-Met. Compound I stood out as the most potent c-Met inhibitor displaying potent inhibitory effects both at enzymic (IC50 = 1.8 nM) and cellular (IC50 = 0.18 μM on EBC-1 cells) levels. In addition, I had a relatively good selectivity compared to a panel of the inhouse 14 RTKs. In the experiment, the researchers used many compounds, for example, 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Category: pyrazoles-derivatives)
1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Category: pyrazoles-derivatives
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics