设计、合成及二取代桂皮酰基羟肟酸脲/硫脲单元作为潜在组蛋白去乙酰化酶抑制剂的生物评价。
Design, synthesis and biological evaluation of di-substituted cinnamic hydroxamic acids bearing urea/thiourea unit as potent histone deacetylase inhibitors.
机构信息
School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
出版信息
Bioorg Med Chem Lett. 2013 Dec 1;23(23):6432-5. doi: 10.1016/j.bmcl.2013.09.051. Epub 2013 Sep 25.
A novel class of di-substituted cinnamic hydroxamic acid derivatives containing urea or thiourea unit was designed, synthesized and evaluated as HDAC inhibitors. All tested compounds demonstrated significant HDAC inhibitory activities and anti-proliferative effects against diverse human tumor cell lines. Among them, 7l exhibited most potent pan-HDAC inhibitory activity, with an IC50 value of 130 nM. It also showed strong cellular inhibition against diverse cell lines including HCT-116, MCF-7, MDB-MB-435 and NCI-460, with GI50 values of 0.35, 0.22, 0.51 and 0.48 μM, respectively.
设计、合成并评价了一类新型的二取代肉桂酰基羟肟酸衍生物，其中含有脲或硫脲单元，作为 HDAC 抑制剂。所有测试的化合物均表现出显著的 HDAC 抑制活性和对多种人肿瘤细胞系的抗增殖作用。其中，化合物 7l 表现出最强的泛 HDAC 抑制活性，IC50 值为 130 nM。它对包括 HCT-116、MCF-7、MDB-MB-435 和 NCI-460 在内的多种细胞系也表现出强烈的细胞抑制作用，GI50 值分别为 0.35、0.22、0.51 和 0.48 μM。
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