Design and Synthesis of Some New Quinoxaline-1,2,4-triazole-3-amide Conjugates as Anticancer Agents
摘要
The newly synthesized quinoxaline-1,2,4-triazole-3-amide conjugates through a multistep method. The prepared compounds were screened for their anticancer activity against secreted human cancer cell lines such as DU-145 (prostate), MCF-7 (breast), and A549 (lung) by applying the MTT method, and the standard drug etoposide was used as a reference drug. The activity results show that two compounds, namely 3,5-dimethoxy-N-(5-{[2-oxoquinoxalin-1(2H)-yl]methyl}-4H-1,2,4-triazol-3-yl)benzamide and 4-methoxy-N-(5-{[2-oxoquinoxalin-1(2H)-yl]methyl}-4H-1,2,4-triazol-3-yl)benzamide exhibited more potent activity than the standard drug. Whereas, two compounds, 3-methoxy-N-(5-{[2-oxoquinoxalin-1(2H)-yl]methyl}-4H-1,2,4-triazol-3-yl)benzamide, and 3,4-dimethoxy-N-(5-{[2-oxoquinoxalin-1(2H)-yl]methyl}-4H-1,2,4-triazol-3-yl)benzamide showed very similar activity against tested cell lines to that of the standard drug IC50 value. The in vitro tyrosine kinase EGFR inhibitory activity results indicate that two compounds, 3,5-dimethoxy-N-(5-{[2-oxoquinoxalin-1(2H)-yl]methyl}-4H-1,2,4-triazol-3-yl)benzamide and 4-methoxy-N-(5-{[2-oxoquinoxalin-1(2H)-yl]methyl}-4H-1,2,4-triazol-3-yl)benzamide exhibited more activity than the standard drug etoposide.