In vitro cytotoxic investigation of some synthesized 1,6-disubstituted-1-azacoumarin derivatives as anticancer agents

In this study, novel synthesized 1,6-disubstituted-1-azacoumarin-3-carboxylic acid derivatives were designed, synthesized and evaluated as potential anticancer agents. The cytotoxicity of novel 1-azacoumarin-3-carboxylic acid derivatives was tested using an MTT assay. High potency was shown by DNA flow cytometry on MCF-7 cells for compound . In addition, topoisomerase IIβ, caspase 3/7, Bax and Bcl-2 enzymes were used to study apoptotic activity. In the same studies, molecular docking analysis assessed activity. Cytotoxicity screening identified multiple bioactive compounds, especially compound . Analysis of DNA flow cytometry revealed that compound exhibited cell cycle arrest. Compound had an increase in the expression of Bax/Bcl-2 ratio and caspase 3/7, and a decrease in topoisomerase IIβ enzyme inhibition.