Деякі фармакологічні властивості 4-[3-(5-бромо-2-гідроксифеніл)-5-феніл-3,4-дигідропіразол-2-іл]-5Н-тіазол-2-ону
A series of 3,5-diaryl pyrazolyl thiazolinones were designed and synthesized as potential biologically 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 activity against a pa...
Збережено в:
| Дата: | 2020 |
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| Автор: | |
| Формат: | Стаття |
| Мова: | English |
| Опубліковано: |
V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine
2020
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| Теми: | |
| Онлайн доступ: | https://bioorganica.com.ua/index.php/journal/article/view/40 |
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| Назва журналу: | Ukrainica Bioorganica Acta |
Репозитарії
Ukrainica Bioorganica Acta| Резюме: | A series of 3,5-diaryl pyrazolyl thiazolinones were designed and synthesized as potential biologically 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 activity against a panel of cancer cells with the lowest growth inhibition concentration (GI50) towards leukemic cell line SR (0.0351 µМ) and ovarian cancer cell line OVCAR-3 (0.248 µМ). It was also found that pyrazolyl thiazolinone 1 inhibited growth of Trypanosoma brucei brucei 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 3T3 in 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 a disintegration of the cell membrane, inhibition of mitochondrial and lysosomal activity, and proliferation of cancer cells. The highest selectivity were detected in the LDH assay |
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