Chromanone Derivatives: Evaluating Selective Anticancer Activity Across Human Cell Lines

Abstract

This study systematically evaluates the cytotoxic effects of chromanone derivatives on a range of human cell lines, including cancerous (MCF-7, DU-145, A549) and normal (SV-HUC-1) types. Using MTT assays, flow cytometric DNA analysis, and Annexin V staining, we assessed the impact of these derivatives on cell viability and apoptosis. Results indicate that the studied compounds exhibit diverse cytotoxic profiles across different cell lines. Notably, compounds in Group B showed enhanced selectivity for cancer cells over normal cells, with significantly lower IC50 values against MCF-7, DU-145, and A549 cells compared to the normal SV-HUC-1 cells. In contrast, the chromanone derivatives from Group A demonstrated comparable cytotoxicity between cancer and normal cells, indicating a lack of selectivity. Specifically, 3-chlorophenylchromanone derivative with 2-methylpyrazoline (B2) exhibited strong cytotoxicity against A549 cells, while demonstrating reduced efficacy in MCF-7, DU-145 and SV-HUC-1 cells. Additionally, structural variations such as halogen substitutions (Cl vs. Br) played a crucial role in modulating the activity of these compounds. These findings suggest that further optimization of substituent types and positions could enhance the selectivity and effectiveness of these compounds as potential anticancer agents. The study provides a foundation for future research aimed at developing targeted therapies with improved cancer cell selectivity and reduced toxicity to normal tissues.