Synthesis and biological activities of new phthalimide and thiazolidine derivatives

Autor: Marina R. Galdino-Pitta, André Silva Lira de Lucena, Douglas Carvalho Francisco Viana, Ivan da Rocha Pitta, Maira Galdino da Rocha Pitta, Marcel L. Almeida, Flaviana Alves dos Santos, Michelly Cristiny Pereira, Vitor A. S. Silva, Moacyr Jesus Barreto de Melo Rêgo
Rok vydání: 2021
Předmět:
Zdroj: Medicinal Chemistry Research. 31:108-119
ISSN: 1554-8120
1054-2523
DOI: 10.1007/s00044-021-02821-7
Popis: 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.
Databáze: OpenAIRE
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