Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects.

Objective: Cancer chemotherapy for the discovery of new antineoplastic drugs is one of the updated areas of medical and pharmaceutical research. Methods: In the current project, a novel series of 1,3-thiazole derivatives were synthesized and their corresponding anticancer activity was evaluated by MTT assay using three cancer cell lines. A2780 (ovarian cancer), PC3 (prostatic carcinoma), and MCF-7 (breast cancer) were utilized for this purpose. Subsequently, Caspase-3 activation, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were also explored for some selected active compounds. Results and Discussion: Fortunately, tested compounds were so active against MCF-7 cells compared to other cell lines. Compounds (VI), (VII), (VIII), (IX), and (XII) enhanced Caspases-3 activity in the MCF-7 cell line that 3-Cl analog (VII) was illustrated as the most cytotoxic index against MCF-7 cells. This is while that among the above analogs (VI–IX), and (XII), just and just, 2-F derivative (IV) revealingly reduced the mitochondrial membrane potential (MMP). The current compounds demonstrated better anticancer activity compared to the other thiazole derivatives. Generally, derivatives bearing electron-withdrawing as well as electron-donating groups are active toward cancerous cell lines. Conclusions: The novel 1,3-thiazole derivatives presented in the current paper could be suggested as potential anticancer agents, especially against breast cancer. [ABSTRACT FROM AUTHOR]