Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives

Journal of Enzyme Inhibition and Medicinal Chemistry
Nazar TrotskoMonika Wujec

Abstract

In our present research, we synthesised new thiazolidine-2,4-diones (12-28). All the newly synthesised compounds were evaluated for antiproliferative and antibacterial activity. Antiproliferative evaluation was carried out using normal human skin fibroblasts and tumour cell lines: A549, HepG2, and MCF-7. The IC50 values were determined for tested compounds revealing antiproliferative activity. Moreover, safety index (SI) was calculated. Among all tested derivatives, the compound 18 revealed the highest antiproliferative activity against human lung, breast, and liver cancer cells. More importantly, the derivative 18 showed meaningfully lower IC50 values when compared to the reference substance, irinotecan, and relatively high SI values. Moreover, newly synthesised compounds were screened for the bacteria growth inhibition in vitro. According to our screening results, most active compound was the derivative 18 against Gram-positive bacteria. Therefore, it may be implied that the novel compound 18 appears to be a very promising agent for anticancer treatment.

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Citations

Oct 21, 2018·Medicinal Research Reviews·Violeta Carmona-MartínezPilar García-Peñarrubia
May 18, 2019·Zeitschrift Für Naturforschung. C, a Journal of Biosciences·Monika StomporJoanna Wietrzyk
May 2, 2020·Journal of Enzyme Inhibition and Medicinal Chemistry·Zohor Mohammad Mahdi AlzhraniSyed Nazreen
Apr 28, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nazar TrotskoMonika Wujec
May 13, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mihaela Ileana Ionescu, Ovidiu Oniga
Jan 2, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rakia Abd AlhameedFernando Albericio
Mar 25, 2020·Topics in Current Chemistry·Nusrat SahibaShikha Agarwal
Aug 24, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nazar TrotskoKatarzyna Dzitko
Feb 16, 2021·European Journal of Medicinal Chemistry·Nazar Trotsko

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