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

authors

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

keywords

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

document type

abstract

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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