Design, Synthesis and Biological Evaluation of Novel Coumarin-Based Hydroxamate Derivatives as Histone Deacetylase (Hdac) Inhibitors with Antitumor Activities

Design, Synthesis and Biological Evaluation of Novel Coumarin-Based Hydroxamate Derivatives as Histone Deacetylase (Hdac) Inhibitors with Antitumor Activities
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具有抗肿瘤活性的新型香豆素基异羟肟酸酯衍生物作为组蛋白脱乙酰酶 (Hdac) 抑制剂的设计、合成和生物学评价

DOI:
10.3390/molecules24142569
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发表时间:
2019-07
期刊:
影响因子:
4.6
通讯作者:
Zhang Hua
Zhang Hua
中科院分区:
化学2区
文献类型:
--
作者:
Yang Feifei;Zhao Na;Song Jiali;Zhu Kongkai;Jiang Cheng shi;Shan Peipei;Zhang Hua

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设计并合成了一系列以香豆素为基础的羟肟酸衍生物作为组蛋白去乙酰化酶抑制剂。选择性化合物对HDAC具有较强的抑制作用,IC50值为nM,最佳化合物(10e)的IC50值接近90倍
A series of novel coumarin-based hydroxamate derivatives were designed and synthesized as histone deacetylase inhibitors (HDACis). Selective compounds showed a potent HDAC inhibition with nM IC50 values, with the best compound (10e) being nearly 90 times
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