Benzylidene 2-Aminoimidazolones Derivatives: Synthesis and in Vitro Evaluation of Anti-tumor Carcinoma Activity

抄録

A series of benzylidene 2-aminoimidazolones derivatives were synthesized. Most compounds displayed strong inhibitory activity on the proliferation of human HepG2 cells in vitro. The active compounds were further evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against five human cancer cell lines in vitro. Compound 2b exhibited the strongest antitumor activities with IC₅₀ values ranging from 12.87–17.10 µM which were nearly 1–3.5 fold less than that of 5-FU (IC₅₀=18.39–56.12 µM) in vitro. Furthermore, compound 2b 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 benzylidene 2-aminoimidazolones derivatives for the treatment of cancer.