In vitro Anticancer and Insilico Studies of Quinoxaline-sulfonyl-1,2,4-triazole Hybrids

New quinoxaline-sulfonyl-1,2,4-triazole hybrids were synthesized (5 a-n) via systematic step-wise sequence. Later, the in vitro cytotoxicity screening of all these compounds revealed that 2-((4-morpholino-[1,2,4]triazolo[4,3-a]quinoxalin-1-yl)sulfonyl)-1-(4-nitrophenyl)ethenone (5 b), 1-(4-methoxy phenyl)-2-((4-morpholino-[1,2,4]triazolo[4,3-a]quinoxalin-1-yl)sulfonyl) ethenone (5 d),4-(2-((4-morpholino-[1,2,4]triazolo[4,3-a] quinoxaline-1-yl)sulfonyl)acetyl)benzonitrilen (5 g), 1-(3,4-dichloro phenyl)-2-((4-morpholino[1,2,4]triazolo[4,3-a]quinoxalin-1-yl) sulfonyl) ethenone (5 j) and 1-(2,5-dimethoxyphenyl)-2-((4-morpholino[1,2,4]triazolo[4,3-a]quinoxalin-1-yl)sulfonyl) ethenone (5 k) were found to more active against the four human cancer cell lines like Hep-G2 (liver), A-549 (lung), MCF-7 (breast) and DU-145 (prostate) with IC50 values ranging from 1.95 +/- 1.34 to 9.61 +/- 1.72 mu M, whereas standard drug displayed IC50 values ranging from 1.97 +/- 0.45 to 3.08 +/- 0.13 mu M. Predominately, compound 5 j displayed superior cytotoxicity against all cell lines than the standard etoposide. As well, the insilico studies of compounds 5 b, 5 d, 5 g, 5 j, and 5 k on EGFR receptor revealed that most potent compound 5 j strongly binds to protein EGFR (pdbid:4HJO). Finally, compounds 5 j and 5 g displayed superior inhibitory activity against tyrosine kinase EGFR than the standard erlotinib.