Ukr. Bioorg. Acta 2020, Vol. 15, N2, 40-47.
Some pharmacological properties of 4-[3-(5-bromo-2-hydroxyphenyl)-5-phenyl-3,4-dihydropyrazol-2-yl]-5H-thiazol-2-one
Anna P. Kryshchyshyn-Dylevych
Danylo Halytsky Lviv National Medical University, 69 Pekarska, Lviv, 79010, Ukraine
A series of 3,5-diaryl-pyrazolyl-thiazolidones was designed and synthesized as potential biological active compounds. The study of anticancer activity of 4-[3-(5-bromo-2-hydroxyphenyl)-5-phenyl-3,4-dihydropyrazol-2-yl]-5H-thiazol-2-one 1 revealed its high antiproliferative properties against a panel of cancer cell lines with the lowest growth inhibition concentration (GI50) towards leukemic cell line SR (0.0351 µĚ) and ovarian cancer cell line OVCAR-3 (0.248 µĚ). It was also found that pyrazoline-thiazolidinone 1 inhibited growth of Trypanosomabruceibrucei by 98,8% at a concentration of 10 µg/mL. The in-depth cytotoxicity study of compound 1 on human hepatocellular carcinoma HepG2 cells and non-tumorigenic murine fibroblast Balb/c 3T3in MTT, NRU, TPC and LDH assays showed that normal cells were less sensitive to compound 1 than the cancer cells; its action had led to disintegration of the cell membrane, inhibition of mitochondrial, lysosomal activity and proliferation of cancer cells. The highest selectivity indices were detected in the LDH assay.
pyrazoline-thiazolidinone hybrids, antitumor activity, antitrypanosomal activity, cytotoxicity.
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