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

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 antiproliferative 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 μM for both A549 and U87-MG cell lines. [Display omitted] •24 original ethyl 3-(arylethynyl)quinoxaline-2-carboxylates and pyrido[4,3-b]quinoxalin-1(2H)-ones were synthesized.•7 molecules tested for the inhibitory activities against A549 and U87-MG cell lines.•Compound 2a and 2d containing a 3-ethynyl group on quinoxaline moiety showed IC50 = 3.3 μM for both A549 and U87-MG cell lines.•Compound 2f displayed IC50 of 3.0 μM and 1.9 μM for A549 and U87-MG respectively.