Design, synthesis and evaluation of anticancer activity of novel 2-thioxoimidazolidin-4-one derivatives bearing pyrazole, triazole and benzoxazole moieties

摘要

A novel series of substituted 2?thiohydantoin incorporated with benzoimidazole, pyrazole, triazole and/or benzoxa?zole moieties has been synthesized using (E)?3?[1?(4?bromophenyl)ethylideneamino]?2?thioxoimidazolidin?4?one 1as the key starting material. The key material 1 also, reacted with an acetic anhydride, aromatic aldehydes, secondaryamines, formaldehyde and triethyl orthoformate to give the corresponding acetyl, chalcone, Mannich bases and eth?oxymethylene derivatives, respectively. The structures of the novel compounds were confrmed by spectral data andelemental analysis. The cytotoxic activity of all synthesized compounds was assessed in vitro against human hepato?cellular cancer cell line (HePG?2) and breast carcinoma cell line (MCF?7). The bioassay results revealed that compound14 has the best activity against HePG?2 cell line (IC50= 2.33 μg/mL), while compound 5 has the best activity againstMCF?7 cell line (IC50= 3.98 μg/mL).