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

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 ag...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 2013/10/01, Vol.61(10), pp.1081-1084
Hauptverfasser: Ling, Yong, Wang, Zhi-Qiang, Xiao, You-An, Zhu, Chenyu, Shen, Liucen, Wang, Xue-Min, Hui, Yi, Wang, Xin-Yang
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Sprache:eng
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Zusammenfassung: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 µ M which were nearly 1–3.5 fold less than that of 5-FU (IC50=18.39–56.12 µ M ) 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.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.c13-00340