https://orcid.org/0000-0001-9957-2188
Abstract
Aims: In this study, novel synthesized 1,6-disubstituted-1-azacoumarin-3-carboxylic acid derivatives were designed, synthesized and evaluated as potential anticancer agents. Materials & methods: 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 3b. 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. Results & conclusion: Cytotoxicity screening identified multiple bioactive compounds, especially compound 3b. Analysis of DNA flow cytometry revealed that compound 3b exhibited cell cycle arrest. Compound 3b had an increase in the expression of Bax/Bcl-2 ratio and caspase 3/7, and a decrease in topoisomerase IIβ enzyme inhibition.
Author contributions
Our colleague IM El-Deen prepared the designed compounds with LAA Barakat and M Elbehery for evaluation biological assays. In addition, M A El-Zend assisted in writing the manuscript.
Financial disclosure
The authors have no financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
Competing interests disclosure
The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
Writing disclosure
No writing assistance was utilized in the production of this manuscript.
Availability of data materials
The datasets used and/or analyzed during the current study are available from the corresponding author upon reasonable request.