Design and Synthesis of Some New Quinoxaline Containing 1,3,4-Oxadiazole Hybrids and Evaluation of Their Anti-Cancer Activity

Abstract Herein, we synthesized some new quinoxaline-1,3,4-oxadiazole hybrids (Va–n) and evaluated for their in vitro anticancer potency towards A549 (lung), MCF-7 (breast), HeLa (cervical) and HEK-293 (embryonic kidney) and etoposide acts as a standard drug. Compounds 1-((5-(3,5-dimethoxyphenyl)-1,3,4-oxadiazol-2-yl) methyl) quinoxaline-2(1H)-one, 1-((5-(4-methoxy phenyl)-1,3,4-oxadiazol-2-yl) methyl) quinoxalin-2(1H)-one and 1-((5-(2,4-dimethyl phenyl)-1,3,4-oxadiazol-2-yl) methyl) quinoxalin-2(1H)-one showed promising anticancer activities against four cancer cell lines. Predominantly, the compound 1-((5-(3,5-dimethoxy phenyl)-1,3,4-oxadiazol-2-yl) methyl) quinoxaline-2(1H)-one has shown greater potency against all cell lines than the standard Etoposide with IC50 ranging from 0.93 ± 0.03, 1.95 ± 0.04, 1.87 ± 0.02 and 2.13 ± 0.05 μM. Furthermore, the compounds1-((5-(3,5-dimethoxyphenyl)-1,3,4-oxadiazol -2-yl) methyl) quinoxaline-2(1H)-one and 1-((5-(4-methoxyphenyl)-1,3,4-oxadiazol -2-yl) methyl) quinoxalin-2(1H)-one displayed promising inhibitory activity over tyrosine kinase EGFR when compared with the standard erlotinib.