Synthesis and evaluation of in vitro antiproliferative activity of new ethyl 3-(arylethynyl)quinoxaline-2-carboxylate and pyrido[4,3-b] quinoxalin-1(2H)-one derivatives - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2016

Synthesis and evaluation of in vitro antiproliferative activity of new ethyl 3-(arylethynyl)quinoxaline-2-carboxylate and pyrido[4,3-b] quinoxalin-1(2H)-one derivatives

Résumé

We report a novel series of quinoxaline derivatives from which agents with antiproliferative activity have been identified. Two ethyl 3-(arylethynyl)quinoxaline-2-carboxylates demonstrated substantial anti proliferative activity against both human non-small cell lung carcinoma (A549) and glioblastoma (U87-MG) cell lines. Pyrido[4,3-b]quinoxalin-1(2H)-ones demonstrated poor activity against A549 and U87-MG cell lines. Three of the derivatives in ethyl 3-(arylethynyl)quinoxaline-2-carboxylate series demonstrated substantial antiproliferative activity. The arylethynyl derivative 2a and 2d proved to be the most cytotoxic with an IC50 value of 3.3 mu M for both A549 and U87-MG cell lines. (C) 2016 Elsevier Masson SAS. All rights reserved.
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hal-01460687 , version 1 (07-02-2017)

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Majdi Hajri, Marie-Anne Esteve, Omar Khoumeri, Raoudha Abderrahim, Thierry Terme, et al.. Synthesis and evaluation of in vitro antiproliferative activity of new ethyl 3-(arylethynyl)quinoxaline-2-carboxylate and pyrido[4,3-b] quinoxalin-1(2H)-one derivatives. European Journal of Medicinal Chemistry, 2016, 124, pp.959--966. ⟨10.1016/j.ejmech.2016.10.025⟩. ⟨hal-01460687⟩
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