Ling Yong, Wang Zhi-Qiang, Xiao You-An, Zhu Chenyu, Shen Liucen, Wang Xue-Min, Hui Yi, Wang Xin-Yang
Medical College, Nantong University.
Chem Pharm Bull (Tokyo). 2013;61(10):1081-4. doi: 10.1248/cpb.c13-00340.
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.
合成了一系列亚苄基2-氨基咪唑酮衍生物。大多数化合物在体外对人肝癌HepG2细胞的增殖表现出较强的抑制活性。通过3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法对活性化合物进行了体外抗五种人癌细胞系的进一步评估。化合物2b表现出最强的抗肿瘤活性，其IC₅₀值为12.87 - 17.10 μM，在体外比5-氟尿嘧啶（IC₅₀ = 18.39 - 56.12 μM）低近1 - 3.5倍。此外，化合物2b能以剂量依赖性方式诱导SMMC-7721细胞凋亡。因此，我们的新发现可能为设计用于治疗癌症的新型亚苄基2-氨基咪唑酮衍生物提供一个新的框架。
