5762-66-3Relevant academic research and scientific papers
Fluorogenic Enzyme-Triggered Domino Reactions Producing Quinoxalin-2(1 H)-one-based Heterocycles
Bonnin, Quentin,Chevalier, Arnaud,Dejouy, Garance,Michaudet, Cédric,Picquet, Michel,Renault, Kévin,Romieu, Anthony,Valverde, Ibai E.
, p. 6494 - 6499 (2020/09/02)
A simple and effective biocompatible domino reaction triggered by a model protease and leading to the formation of strongly fluorescent quinoxalin-2(1H)-one N-heterocycles is described. Some positive attributes including versatility and the ability to pro
Quinoxalinone (Part II). Discovery of (Z)-3-(2-(pyridin-4-yl)vinyl)quinoxalinone derivates as potent VEGFR-2 kinase inhibitors
Shi, Leilei,Zhou, Jianfeng,Wu, Jifeng,Cao, Junya,Shen, Yuemao,Zhou, Hua,Li, Xun
, p. 1840 - 1852 (2016/04/05)
Inhibition of VEGFR-2 kinase has been highlighted as one of the well-defined strategies to suppress tumor growth via blockade of angiogenesis. Guided by the principles of bioisosteric replacement and pharmacophoric fragment migration, a series of novel quinoxalinone derivates were designed, synthesized and evaluated for their VEGFR-2 inhibitory potencies. Among them, compounds 7c, 8b, 8c, 8e and 10b displayed antiangiogenic abilities via the in vitro tube formation assay (cellular level) and ex vivo rat aortic ring assay (tissue level) at a low concentration (0.1 μM). By means of in vivo zebrafish embryo model, two (Z)-3-(2-(pyridin-4-yl)vinyl)quinoxalinone derivates 8c and 8e showed significant antiangiogenesis effects, suggesting they have potentials to be developed into antiangiogenesis agents via further structural optimization. Moreover, these two compounds also demonstrated potent inhibition toward VEGFR-2 and B-raf kinases in a low concentration (1 μM). A possible interpretation of our evaluation result has been presented by a molecular docking study by docking representative compound 8c with VEGFR-2.
Fluorescent Products of Reaction between α-Keto Acids and 1,2-Diamino-4,5-dimethoxybenzene
Hara, Shuuji,Yamaguchi, Masatoshi,Nakamura, Masaru,Ohkura, Yosuke
, p. 3493 - 3498 (2007/10/02)
The fluorescent products formed from α-keto acids and 1,2-diamino-4,5-dimethoxybenzene were shown to be the corresponding 3-substituted 6,7-dimethoxy-2(1H)-quinoxalinones.The fluorescence properties of the products are described; they fluorescence most intensely at pH 6.0-8.0.
