Synthesis of Quinoxlines Containing 1,2,3-Triazoles and Their Anti-Bacterial and Anti-Cancer Activity

Abstract A series of 1-((1aryl)-1H-1,2,3-triazol-4-yl)methyl)quinoxalin-2(1H)-ones have been synthesized in moderate to high yields and evaluated for their anti-bacterial and anti-cancer activities. Among all the derivatives tested, the compound 1-((1-(2-fluorophenyl)-1H-1,2,3-triazol-4-yl)methyl)quinoxalin-2(1H)-one exhibited most potent anti-bacterial activity against B. subtilis and S. epidermidis with and also demonstrated comparable inhibitory activity against S. aureus to that of the standard streptomycin. Also, compound 1-((1-(2,4-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methyl)quinoxalin-2(1H)-one effectively inhibited the gram-positive S. epidermidis equal to that of the standard streptomycin and moderate activity against B. subtilis and S. aureus. Furthermore the compound1-((1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)methyl)quinoxalin-2(1H)-one has shown superior activity against E. coli and moderate activity against B. subtilis, S. epidermidis, and S. aureus when compared with positive control. Moreover, all these compounds were screened for their anti-cancer activity against human cancer cell lines via MCF-7 (breast), A-549 (lungs) and HeLa (cervical). In vitro anti-cancer activity reveals that a few compounds exhibited potent inhibitory in a variety of cancer cell lines. Among the compounds 1-((1-(2,4-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)quinoxalin-2(1H)-one shown more potent anti-cancer activity against all tested cancer cell lines compared to standard drug, the remaining compounds1-((1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)methyl)quinoxalin2(1H)-one and 1-((1-(2,4-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methyl)quinoxalin-2(1H)-one exhibited promising anti-cancer activity compared to the other tested compounds.