《Design, synthesis and biological evaluation of novel 1H-1,2,4-triazole, benzothiazole and indazole-based derivatives as potent FGFR1 inhibitors via fragment-based virtual screening》 was written by Liu, Jian; Wen, Yu; Gao, Lina; Gao, Liang; He, Fengjun; Zhou, Jingxian; Wang, Junwei; Dai, Rupeng; Chen, Xiaojing; Kang, Di; Hu, Lihong. Related Products of 403-33-8 And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020. The article conveys some information:
Fibroblast growth-factor receptor (FGFR) is a potential target for cancer therapy. We designed three novel series of FGFR1 inhibitors bearing indazole, benzothiazole, and 1H-1,2,4-triazole scaffold via fragment-based virtual screening. All the newly synthesized compounds were evaluated in vitro for their inhibitory activities against FGFR1. Compound 9d (I) bearing an indazole scaffold was first identified as a hit compound, with excellent kinase inhibitory activity (IC50 = 15.0 nM) and modest anti-proliferative activity (IC50 = 785.8 nM). Through two rounds of optimization, the indazole derivative 9u (II) stood out as the most potent FGFR1 inhibitors with the best enzyme inhibitory activity (IC50 = 3.3 nM) and cellular activity (IC50 = 468.2 nM). Moreover, II also exhibited good kinase selectivity. In addition, mol. docking study was performed to investigate the binding mode between target compounds and FGFR1. In addition to this study using Methyl 4-fluorobenzoate, there are many other studies that have used Methyl 4-fluorobenzoate(cas: 403-33-8Related Products of 403-33-8) was used in this study.
Methyl 4-fluorobenzoate(cas: 403-33-8) can be used in the synthesis of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH2-substituted benzyl moiety.Related Products of 403-33-8
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