engleski

Anti-proliferative effects of novel hybrids of 1, 2, 3-triazole-pyrimidines, 1, 2, 3–triazole–benzimidazoles and 1, 2, 3-triazole-coumarins

The series of novel hybrids including: 1, 2, 3-triazole-pyrimidines, 1, 2, 3-triazole-coumarins and 1, 2, 3-triazole benzimidazoles were evaluated for their anti-proliferative activity against five human cancer cell lines and normal embryo mouse fibroblasts. Among these, TG-16 (C16H12ClN5 ; IC50=4, 83µM), TG-14 (C22H15BrF2N8O2 ; IC50=4, 53µM) and TG-15 (C22H15BrCl2N8O2 ; IC50=1µM) exerted the most potent cytostatic activity in lung, pancreatic and hepatocellular carcinoma cell lines, respectively. Interestingly, the most selective anticancer effects were observed with compounds MM-11(C17H14FN5) and MM-19 (C17H14FN5) in lung carcinoma cells with IC50=4, 78 µM and IC50=7, 79 µM, respectively. Additional in vitro toxicity studies revealed mitochondrial impairment as a primary mechanism accounting for observed cytotoxic effects of TG-16, MM-11 and MM-19. The latter also showed strong in vitro renal toxicity.

1; 2; 3-triazole-pyrimidines; 1; 2; 3-triazole-coumarins and 1; 2; 3-triazole benzimidazoles; human cancer cell lines

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