Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities
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开发具有抗肿瘤活性的含有 1,2,4-恶二唑部分核心的基于异羟肟酸酯的组蛋白脱乙酰酶抑制剂
DOI：
10.1016/j.bmcl.2018.11.027
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发表时间：
2019
影响因子：
2.7
通讯作者：
Zhang Hua
中科院分区：
文献类型：
--
作者：
Yang Feifei;Shan Peipei;Zhao Na;Ge Di;Zhu Kongkai;Jiang Cheng shi;Li Peifeng;Zhang Hua
Histone deacetylases (HDACs) has proved to be promising target for the development of antitumor drugs. In this study, we reported the design and synthesis of a class of novel hydroxamate-based bis-substituted aromatic amide HDAC inhibitors with 1,2,4-oxadiazole core. Most newly synthesized compounds displayed excellent HDAC1 inhibitory effects and significant anti-proliferative activities. Among them, compounds11aand11cincreased acetylation of histone H3 and H4 in dose-dependent manner. Furthermore,11aand11cremarkably induced apoptosis in HepG2 cancer cells. Finally, the high potency of compound11awas rationalized by molecular docking studies.
