Synthesis and Characterization of Novel 4-aryl-4 H-chromene Derivatives using Borax and Evaluation of their Anticancer Effects

Abstract

Background/introduction: 4-aryl-4H-chromenes have attracted attention as potential anticancer agents.

Objective: In an effort to discover effective compounds, we designed a new series of these chromenes with methoxy substitution at 2, 3, 4, 5, and 6 positions.

Methods: The synthesized compounds were tested for anticancer properties against two human cancer cell lines (MCF- 7 and PC3) as well as a normal cell line. Furthermore, induction of apoptosis was explored through various methods, such as flow cytometry analysis, morphological changes, activation of caspase 3, ROS, and MMP.

Results: The MTT assay showed that the 5g derivative, with methoxy groups at ortho and meta positions, exhibited the highest potency (IC₅₀ = 40 μM) against the PC3 cell line. Our findings revealed that compound 5g induced apoptosis in the PC3 cell line, which was demonstrated by activation of caspase 3, an increase in ROS levels, and early apoptosis percentage.

Conclusion: These results suggest that compound 5g holds promise as a potential therapeutic approach to cancer treatment.

Keywords: Chromenes; antiproliferative activity; antitumor activity; apoptosis; biological activity; cytotoxicity.