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Ukr. Bioorg. Acta 2020, Vol. 15, N1, 2-11

Anticancer Evaluation of Di- and Trifunctional Substituted 1,3-Thiazoles

Kostyantyn V. Turov, Îleg P. Mitiukhin, Svitlana A. Chumachenko, Vladimir S. Zyabrev, Volodymyr S. Brovarets*

V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine, 1, Murmanska St., Kyiv, 02094, Ukraine.
e-mail: brovarets@bpci.kiev.ua

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 C
2 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).

1,3-thiazole; anticancer activity; growth inhibitor; cytostatic activity; cytotoxic activity

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