Synthesis and in vitro biological evaluation of novel 2-aminoimidazolone derivatives as anti-tumor agents

Novel 2-aminoimidazolone derivatives were synthesized. Most compounds displayed strong anticancer activities against human carcinoma cells in vitro. Compounds 8a, 8b and 8j exhibited optimal activity superior to 5-FU in most cancer cells tested. Especially, the IC50s of 8b (12.6–21.5 μmol/L) against five tumor cells were 1–4 fold less than those of 5-FU (18.4–56.1 μmol/L) in vitro. Furthermore, compound 8b could induce SMMC-7721 cell apoptosis in a dose-dependent manner. Therefore, our novel findings may provide a new framework for the design of new 2-aminoimidazolone derivatives for the treatment of cancer.

Graphical abstractNovel 2-aminoimidazolones derivatives were synthesized. Compound 8b exhibited the strongest antitumor activities and induced SMMC-7721 cell apoptosis in a dose-dependent manner.Figure optionsDownload full-size imageDownload as PowerPoint slide