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Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
Ist Teil von
Journal of enzyme inhibition and medicinal chemistry, 2018-01, Vol.33 (1), p.17-24
Ort / Verlag
England: Taylor & Francis
Erscheinungsjahr
2018
Quelle
MEDLINE
Beschreibungen/Notizen
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 IC
50
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 IC
50
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.