Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship was written by Zhang, Ning;Yu, Zhimei;Yang, Xiaohong;Zhou, Yan;Tang, Qing;Hu, Ping;Wang, Jia;Zhang, Shao-Lin;Wang, Ming-Wei;He, Yun. And the article was included in European Journal of Medicinal Chemistry in 2018.Recommanded Product: 365564-07-4 This article mentions the following:
Phosphatidylinositol 3-kinase α (PI3Kα) is the most frequently mutated kinase in human cancers, making it an attractive therapeutic target for cancer treatment. The authors identified a structurally novel PI3Kα H1047R mutant inhibitor Hit-01 (5,7-dichloro-2,3-di(furan-2-yl)quinoxaline) (EC50 = 76.0 μM) through a high-throughput screening campaign. Chem. optimizations enabled the authors to discover compound 7b (6-bromo-7-(2-fluorophenyl)-2,3-di(furan-2-yl)quinoxaline), which strongly inhibited PI3Kα H1047R mutant with an EC50 value of 0.137 μM, over 500-fold more potent than Hit-01. Western blotting anal. suggested that 7b could decrease the phosphorylation level of p-AKT, another proof that 7b inhibited PI3Kα H1047R function. Cell viability assay revealed that 7b inhibited HCT116 cancer cell growth with an IC50 value of 11.23 μM. In addition, 7b was found to arrest cell cycle at G1 phase and induce cell apoptosis via up-regulation of caspase-3, caspase-8 and caspase-9 protein expressions. Collectively, all these data demonstrated that 7b could be a promising lead for the development of structurally novel PI3Kα inhibitors. In the experiment, the researchers used many compounds, for example, 2-(3,5-Dimethoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (cas: 365564-07-4Recommanded Product: 365564-07-4).
2-(3,5-Dimethoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (cas: 365564-07-4) belongs to ethers. Of all the functional groups, ethers are the least reactive ones. Ether bonds are quite stable towards bases, oxidizing agents and reducing agents. Ethyl ether is an excellent solvent for extractions and for a wide variety of chemical reactions. It is also used as a volatile starting fluid for diesel engines and gasoline engines in cold weather. Dimethyl ether is used as a spray propellant and refrigerant. Methyl t-butyl ether (MTBE) is a gasoline additive that boosts the octane number and reduces the amount of nitrogen-oxide pollutants in the exhaust. The ethers of ethylene glycol are used as solvents and plasticizers.Recommanded Product: 365564-07-4
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem