Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold was written by Wang, Ming-Shu;Zhuo, Lin-Sheng;Yang, Fan-Peng;Wang, Wen-Jie;Huang, Wei;Yang, Guang-Fu. And the article was included in European Journal of Medicinal Chemistry in 2020.Recommanded Product: Ethyl 2-(4-fluorophenyl)acetate This article mentions the following:
A potent and novel MET inhibitor, naphthyridin-4(1H)-one derivatives I and II [R1 = Me, cyclopropyl, Bu, etc.; R2 = H, Me, Et, 2-hydroxyethyl, 2-hydroxy-2-methylpropyl] was synthesized via a scaffold-hopping strategy of a 2,7-naphthyridinone MET kinase inhibitor III. Lead compound I had good potency (IC50 of 9.8 nM), but unfavorable pharmacokinetic profiles (F = 12%, CL = 5.0 L/h/kg). Systematic structural optimization of compound I resulted in II [R1 = cyclopropyl, R2 = H] (MET, IC50 = of 9.8 nM) with a comparable MET potency to that of compound IV and a favorable pharmacokinetic profile (F = 63%, CL = 0.12 L/h/kg). Further study of the derivatization of N(1) amine group of II [R1 = cyclopropyl, R2 = H] led to the discovery of compound II [R1 = cyclopropyl, R2 = Me] with good MET potency (IC50 of 7.1 nM), promising VEGFR-2 selectivity (3226-fold) and a markedly drug-likeness improvement (F = 57.7%, CL = 0.02 L/h/kg). The excellent VEGFR-2 selectivity and favorable drug-likeness of II [R1 = cyclopropyl, R2 = Me] suggested that the 1,6-naphthyridine moiety could be used as a new scaffold for kinase inhibitor discovery. In the experiment, the researchers used many compounds, for example, Ethyl 2-(4-fluorophenyl)acetate (cas: 587-88-2Recommanded Product: Ethyl 2-(4-fluorophenyl)acetate).
Ethyl 2-(4-fluorophenyl)acetate (cas: 587-88-2) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Recommanded Product: Ethyl 2-(4-fluorophenyl)acetate
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Ester – an overview | ScienceDirect Topics