Evaluation of Cytotoxicity of 2-(4-phenylthiazol-2-yl) benzo[de]isoquinoline-1,3-dione Derivatives

Abstract

Background and Objective: This study aims to evaluate the cytotoxic effects of 2-(4-phenylthiazol-2-yl) benzo[de]isoquinoline-1,3-dione derivatives. These compounds were investigated for their potential to induce apoptosis in fibroblast, KB, MCF-7, and PC3 cell lines.

Materials and Methods: The cytotoxicity of the synthesized derivatives was assessed on fibroblast, KB, MCF-7, and PC3 cell lines using the MTT assay. Additionally, mitochondrial membrane potential and reactive oxygen species (ROS) levels were measured in these cells. Data were analyzed using Prism software.

Results: Among methoxy-substituted derivatives at meta and para positions, the para-methoxy substituted compound exhibited higher cytotoxicity against fibroblast cells with an IC50 of 9.5 ± 0.004 µM compared to the meta-substituted derivative. This increased toxicity is attributed to the electron-donating capacity of the para-methoxy group, which facilitates electron donation to the aromatic rings. In the KB cell line, the derivative bearing a para-methyl substituent showed significant cytotoxicity with an IC50 of 8.3 ± 0.005 µM. Both para-methoxy and para-methyl derivatives demonstrated acceptable cytotoxic effects against MCF-7 cells.

Conclusion: The methyl substituent, acting as an electron-donating group, exhibited notable cytotoxicity against the tested cell lines. Based on these in vitro anti-cancer findings, further studies are recommended to evaluate the effects of these derivatives on caspase activity and to explore their cytotoxic potential against other cancer cell lines.