36818-07-2Relevant articles and documents
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors
Oyallon, Bruno,Brachet-Botineau, Marie,Logé, Cédric,Bonnet, Pascal,Souab, Mohamed,Robert, Thomas,Ruchaud, Sandrine,Bach, Stéphane,Berthelot, Pascal,Gouilleux, Fabrice,Viaud-Massuard, Marie-Claude,Denevault-Sabourin, Caroline
, p. 101 - 109 (2018)
We identified a new series of quinoxaline-2-carboxylic acid derivatives, targeting the human proviral integration site for Moloney murine leukemia virus-1 (HsPim-1) kinase. Seventeen analogues were synthesized providing useful insight into structure-activity relationships studied. Docking studies realized in the ATP pocket of HsPim-1 are consistent with an unclassical binding mode of these inhibitors. The lead compound 1 was able to block HsPim-1 enzymatic activity at nanomolar concentrations (IC50 of 74 nM), with a good selectivity profile against a panel of mammalian protein kinases. In vitro studies on the human chronic myeloid leukemia cell line KU812 showed an antitumor activity at micromolar concentrations. As a result, compound 1 represents a promising lead for the design of novel anticancer targeted therapies.
A highly selective fluorescent chemosensor for Mg2+ based on a diarylethene with a quinoxaline unit
Zhang, Yaping,Li, Hui,Jiang, Duohua,Pu, Shouzhi
, (2020)
A new fluorescent probe 1O was synthesized through linking diarylethene and Quinoxaline-2-hydraqzide group, probe 1O showed a selective “off-on” fluorescent response toward Mg2+. In the presence of Mg2+, the probe 1O displayed a distinct change of fluorescence color, from dark to green, the fluorescence intensity increased 6.8-fold, and meanwhile, emission peak has a significant blue shift, which was shifted from 524 nm to 518 nm. Then, on account of the fluorescence properties of compound 1O, we designed a logic gate. On top of that, probe 1O also can be successfully used to monitor Mg2+ of the actual water samples.
3-Arylamino-quinoxaline-2-carboxamides inhibit the PI3K/Akt/mTOR signaling pathways to activate P53 and induce apoptosis
Chen, Nan-Ying,Lu, Ke,Yuan, Jing-Mei,Li, Xiao-Juan,Gu, Zi-Yu,Pan, Cheng-Xue,Mo, Dong-Liang,Su, Gui-Fa
, (2021/06/30)
Thirty-eight new 3-arylaminoquinoxaline-2-carboxamide derivatives were in silico designed, synthesized and their cytotoxicity against five human cancer cell lines and one normal cells WI-38 were evaluated. Molecular mechanism studies indicated that N-(3-A
2-(omega-dialkylamino)aminoalkyl-3-aryloxazolequinoxaline compounds as well as preparation method and application thereof
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Paragraph 0060; 0061; 0062, (2018/09/26)
The invention discloses 2-(omega-dialkylamino)aminoalkyl-3-aryloxazolequinoxaline compounds as well as a preparation method and application thereof, and specially relates to a pharmaceutical composition containing the compounds, and an application in preparation of antitumor and topoisomerase I inhibiting drugs. The compounds disclosed by the invention have a good inhibitory effect on topoisomerase I, and exhibit good antitumor effects in vitro and in vivo.