Design, Synthesis, and Antiproliferative Activity of Novel Flavone Derivatives

Background Cancer is a complex disease in which some of the cells grow uncontrollably and spread to other parts of the body. Objective The present study focuses on molecular docking and synthesis of novel flavone derivatives substituted with heterocyclic rings. Methods The anticancer activity of novel flavones against human aromatase enzyme using human breast cancer cell line MCF-7 through MTT assay was demonstrated. The synthesized compounds for the determination of single or double-strand DNA damage through the single-cell electrophoresis/comet assay were evaluated. Results In this study, we found that the derivative 3M with morpholine ring showed the highest anticancer potency against the MCF-7 cell line compared to that of other flavone derivatives. Compound 3T showed less cytotoxicity against the MCF-7 cell line. Conclusion Based on the findings, flavone scaffolds can be selected as a skeleton for the development of heterocyclic amine-containing flavones with the potential to develop as anticancer drugs.