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


  • Hajri Majdi
  • Esteve Marie-Anne
  • Khoumeri Omar
  • Abderrahim Raoudha
  • Terme Thierry
  • Montana Marc
  • Vanelle Patrice


  • Structure-activity relationship
  • Tdae strategy
  • Cell-lines
  • Assay
  • Antitumor activity
  • Reactivity
  • Quinoxaline
  • Series
  • Organic chemistry

document type



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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