In Vitro Cytotoxicity of Benzopyranone Derivatives with Basic Side Chain Against Human Lung Cell Lines

Abstract

Background: Coumarins belong to an important group of useful drugs with diverse pharmacological properties. In the present study, the in vitro cytotoxicity of new coumarin-based benzopyranone derivatives containing diethylaminoethoxy (5), dimethylaminoethoxy (6), morpholinoethoxy (7), piperidinylethoxy (8) and pyrrolidinylethoxyl (9) amino side chain against human carcinoma (A549) and normal (LL47) lung cell lines was evaluated. Materials and Methods: The cytotoxicity was evaluated by crystal violet dye binding assay. The effect of compound 9 on different phases of the cell cycle was determined using flow cytometry. Results: In A549 cells, the 50% lethal dose (LD₅₀) for compounds 5-9 were found to be 7.08, 5.0, 34.2, 8.33 and 5.83 μM, respectively, while in LL47 cells, the LD₅₀ values were found to be 16.7, 20.4, 34.6, 15.4 and 8.75 μM, respectively after 48 h treatment. Cell cycle data indicated that A549 cells were arrested at different phases depending on the concentration. Conclusion: Compounds 5-9 showed anticancer activity against lung cancer cell lines, while compound 6 showed highly selective anticancer activity.