Anticancer evaluation of di- and trifunctional substituted 1,3-thiazoles

Abstract

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).