作者
Fang Wang, Wen Lu, Tao Zhang, Jinyun Dong, Hongping Gao, Pengfei Li, Sicen Wang, Jie Zhang
发表日期
2013/11/15
期刊
Bioorganic & medicinal chemistry
卷号
21
期号
22
页码范围
6973-6980
出版商
Pergamon
简介
Histone deacetylase inhibitors (HDACIs) offer a promising strategy for cancer therapy. The discovery of potent ferulic acid-based HDACIs with hydroxamic acid or 2-aminobenzamide group as zinc binding group was reported. The halogeno-acetanilide was introduced as novel surface recognition moiety (SRM). The majority of title compounds displayed potent HDAC inhibitory activity. In particular, FA6 and FA16 exhibited significant enzymatic inhibitory activities, with IC50 values of 3.94 and 2.82 μM, respectively. Furthermore, these compounds showed moderate antiproliferative activity against a panel of human cancer cells. FA17 displayed promising profile as an antitumor candidate. The results indicated that these ferulic acid derivatives could serve as promising lead compounds for further optimization.
引用总数
201420152016201720182019202020212022202320243465641425
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