1095200-47-7Relevant academic research and scientific papers
One-step approach for the synthesis of functionalized quinoxalines mediated by T3P-DMSO or T3P: Via a tandem oxidation-condensation or condensation reaction
Harsha, Kachigere B.,Rangappa, Kanchugarkoppal S.
, p. 57154 - 57162 (2016)
An easy and efficient propylphosphonic anhydride (T3P)-DMSO or T3P mediated oxidation-condensation or condensation reaction for the synthesis of quinoxalines derived from the interaction of different arrays of condensing partners with ortho-phenylene diamines (o-PDs) under simple and mild reaction conditions in one step has been reported for the first time.
Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship
Zhang, Ning,Yu, Zhimei,Yang, Xiaohong,Zhou, Yan,Tang, Qing,Hu, Ping,Wang, Jia,Zhang, Shao-Lin,Wang, Ming-Wei,He, Yun
, p. 37 - 49 (2018)
Phosphatidylinositol 3-kinase α (PI3Kα) is the most frequently mutated kinase in human cancers, making it an attractive therapeutic target for cancer treatment. We identified a structurally novel PI3Kα H1047R mutant inhibitor Hit-01 (EC50 = 76.0 μM) through a high-throughput screening campaign. Chemical optimizations enabled us to discover compound 7b, which strongly inhibited PI3Kα H1047R mutant with an EC50 value of 0.137 μM, over 500-fold more potent than Hit-01. Western blotting analysis 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.
Gallium(III) triflate-catalyzed synthesis of quinoxaline derivatives
Cai, Jing-Jing,Zou, Jian-Ping,Pan, Xiang-Qiang,Zhang, Wei
supporting information; scheme or table, p. 7386 - 7390 (2009/05/07)
Gallium(III) triflate-catalyzed reactions of phenylene-1,2-diamines and 1,2-diketones produce quinoxalines in excellent to quantitative yields. The reactions proceed with 1 mol % catalyst in ethanol at room temperature. The catalyst can be recycled for at
