Design, Synthesis and Anticancer Activity of New Benzofuran‐Chalcone Hybrids and Their Water Soluble Sodium Salts

Abstract In this study, firstly, 1‐(7‐ethoxy‐1‐benzofuran‐2‐yl) ethanone and 1,1’‐(7‐ethoxy‐1‐benzofuran‐2,4‐diyl)diethanone were synthesized for the starting reagent purposes. The synthesized benzofuran‐chalcone salts were soluble in water at room temperature. Structural analysis of the synthesized compounds was characterized by elemental analysis, FT‐IR and NMR spectroscopy techniques. The anticancer activities of the compounds were determined by SRB viability assay in human lung cancer (A549, H1299) and breast cancer (MCF‐7, MDA‐MB‐231) cell lines. Findings for apoptosis were determined by flow cytometry analysis and the PARP‐ELISA method. The results of the in vitro SRB analysis of the compounds showed that some of the chalcone hybrids were very effective on both types of cancer in a dose and time‐dependent manner. Treatment of all cancer cell types with these hybrids resulted in a significant increase in the percentage of early and mainly late apoptotic cells, demonstrating their apoptosis‐inducing effects via the Caspase 3/7 Activity.