Synthesis and biological activities of new phthalimide and thiazolidine derivatives

Abstract

The combination of pharmacophoric nuclei with different targets has been a strategy for the development of new drugs aimed at improving cancer treatment. A series of ten novel phthalimido-thiazolidine-2-4-dione derivatives were synthesized by two different synthetic routes. The compounds were tested and evaluated in vitro, through antineoplastic activities against cancer cells. Cell cycle analysis and clonogenic assay were also performed. The synthesized FT-12 compound (9j) exhibited antiproliferative activity against Panc-1, Sk-mel-28, and PC-3 cells. FT-12 reduced the ability to form new clones, also caused irreversibility in cell cycle, inducing arrest in the S phase. Besides, the compound (FT-12) induced necrosis and apoptosis. The results suggest that phthalimido-thiazolidine derivatives may be useful in cancer therapy, highlighting compound FT-12 (9j) as a promising candidate. However, more studies must be carried out to confirm its viability.

Kinetic Studies, Antioxidant Activities, Enzyme Inhibition Properties and Molecular Docking of 1,3-Dihydro-1,3-Dioxoisoindole Derivatives

“…Phthalimides (1,3-dihydro-1,3-dioxoisoindoles) are a significant class of drugs showing antimicrobial, 1 antibacterial, 2 antituberculosis, 3 cytotoxicity, 4 anticancer, 5 analgesic, 6 acetylcholinesterase inhibitors, 7 an inhibitor of nitric oxide synthase to human neuronal, 8 and antiproliferative. 9 These compound's derivatives showed various biological activities, were substantiated as an exciting pharmacophore and could interact with the peripheral anionic site of the enzymes.…”