Synthesis and biological activities of new phthalimide and thiazolidine derivatives

Synthesis and biological activities of new phthalimide and thiazolidine derivatives

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...

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Bibliographic Details
Published in:Medicinal chemistry research Vol. 31; no. 1; pp. 108 - 119
Main Authors: Santos, Flaviana A., Almeida, Marcel L., Silva, Vitor A. S., Viana, Douglas C. F., Pereira, Michelly C., Lucena, André S. L., Pitta, Maira G. R., Galdino-Pitta, Marina R., de Melo Rêgo, Moacyr J. B., da Rocha Pitta, Ivan
Format: Journal Article
Language:English
Published: New York Springer US 2022
Springer Nature B.V
Subjects:
Apoptosis
Biochemistry
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Cancer
Cell cycle
Diketones
Drug development
Inorganic Chemistry
Medicinal Chemistry
Necrosis
Original Research
Pharmacology/Toxicology
Phthalimide
Phthalimides
S phase
Synthesis
Medicinal Chemistry
Therapeutic innovation
Phthalimide
Cell Death
Cancer
Thiazolidine
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Summary: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.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-021-02821-7