91895-39-5Relevant articles and documents
Design, synthesis, and molecular docking studies of new [1,2,4]triazolo[4,3-a]quinoxaline derivatives as potential A2B receptor antagonists
Ezzat, Hany G.,Bayoumi, Ashraf H.,Sherbiny, Farag F.,El-Morsy, Ahmed M.,Ghiaty, Adel,Alswah, Mohamed,Abulkhair, Hamada S.
, p. 291 - 306 (2020/03/24)
Abstract: Many shreds of evidence have recently correlated A2B receptor antagonism with anticancer activity. Hence, the search for an efficient A2B antagonist may help in the development of a new chemotherapeutic agent. In this article, 23 new derivatives of [1,2,4]triazolo[4,3-a]quinoxaline were designed and synthesized and its structures were confirmed by different spectral data and elemental analyses. The results of cytotoxic evaluation of these compounds showed six promising active derivatives with IC50 values ranging from 1.9 to 6.4?μM on MDA-MB 231 cell line. Additionally, molecular docking for all synthesized compounds was performed to predict their binding affinity toward the homology model of A2B receptor as a proposed mode of their cytotoxic activity. Results of molecular docking were strongly correlated with those of the cytotoxic study. Finally, structure activity relationship analyses of the new compounds were explored. Graphic abstract: [Figure not available: see fulltext.]
Novel [1,2,4]triazolo[4,3-a]quinoxaline amino phenyl derivatives or pharmaceutically acceptable salts thereof, preparation method therof and pharmaceutical composition for use in preventing or treating bromodomain extra-terminal(BET) protein activity related diseases containing the same as an active ingredient
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Paragraph 0291; 0292; 0296; 0297, (2018/12/12)
The present invention refers to [1, 2, 4] triazolo [4, 3 a-a] the [khwi [khwi] roh it was cut aminophenyl derivatives or pharmaceutically acceptable salts, including BET and manufacturing method of active ingredient (bromodomain extra non-terminal) a pharmaceutical composition for preventing or treating protein related disorders are disclosed. The present invention according to [1, 2, 4] triazolo [4, 3 a-a] aminophenyl derivatives of one of the [khwi [khwi] roh it was cut low concentrations in the BET protein family protein and an excellent BRD4 billion number, so that the inducing cytotoxicity against tumor cell lines, BET diseases associated with protein, in particular can be useful in preventing or treating cancer or an autoimmune disease. (by machine translation)
Synthesis and antimicrobial activity of some novel quinoxalines
Soliman,Amer
experimental part, p. 1401 - 1410 (2012/04/04)
2-Hydrazino-3-chloroquinoxaline 2 was prepared and reacted with active methylene compounds, potassium thiocyanate, carbon disulfide, phenylisothiocyanate, acetic acid, ethyl chloroformate, triethyl orthoformate, and Lawessen's reagent (LR) to give a new class of fused quinoxalines 4-16, respectively. Also, 2,3-dihydrazinoquinoxaline 3 was prepared and reacted with carbon disulfide, phenyl isothiocyanate, and triethyl orthoformate to give the corresponding di[1,2,4] triazolo-[4,3-a:3′,4′-c]-quinoxalines 17-19, respectively. Reaction of 3 with LR gave the corresponding di[1,2,4,3] triazophospholo[4,5-a:5′,4′-c]quinoxaline-1,6-dithione (20). It was found that all synthesized compounds exhibit antimicrobial activity and that compound 20 had a broad spectrum of activity. Copyright Taylor & Francis Group, LLC.