Оцінка протиракової активності ди- та трифункціональнозаміщених 1,3-тіазолів

• Дата: 2020
• Автори: Turov, Kostyantyn V., Mitiukhin, Оleg P., Chumachenko, Svitlana A., Zyabrev, Vladimir S., Brovarets, Volodymyr S.
• Формат: Стаття
• Мова: English
• Опубліковано: V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine 2020
• Теми: 1,3-thiazole; anticancer activity; growth inhibitor; cytostatic activity; cytotoxic activity; 1,3-тіазол; протиракова активність; інгібітори росту; цитостатична активність; цитотоксична активність
• Онлайн доступ: https://bioorganica.com.ua/index.php/journal/article/view/2
• Назва журналу: Ukrainica Bioorganica Acta

Anticancer activity of a series of polyfunctional substituted 1,3-thiazoles has been studied within the international scientific program “NCI-60 Human Tumor Cell Lines Screen”. Screening was performed in vitro on 60 cell lines of lungs, kidneys, CNS, ovaries, prostate, and breast cancer, epithelial cancer, leukemia, and melanoma. The most effective compounds were those with a piperazine substituent at C2 of the 1,3-thiazole cycle: 1-(4-((4-methylphenyl)-sulfonyl)-2-phenyl-1,3-thiazol-5-yl)piperazine (average lg GI50 = -5.87, lg TGI = -5.54, lg LC50 = -5.21), 1-(2-(3,5-dimethyl-1H-pyrazol-1-yl)-4-((4-methylpheyl)sulfonyl)-1,3-thiazol-5-yl)piperazine (average lg GI50 = -5.66, lg TGI = -5.26, lg LC50 = -4.83), and 1-(2,4-bis((4-methylphenyl)sulfonyl)-1,3-thiazol-5-yl)piperazine (average lg GI50 = -5.67, lg TGI = -5.21, lg LC5050 = -4.67).