基于硫醇的SAHA类似物作为有效的组蛋白去乙酰化酶抑制剂。
Thiol-based SAHA analogues as potent histone deacetylase inhibitors.
作者信息
Suzuki Takayoshi, Kouketsu Akiyasu, Matsuura Azusa, Kohara Arihiro, Ninomiya Shin-Ichi, Kohda Kohfuku, Miyata Naoki
机构信息
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Aichi, Nagoya 467-8603, Japan.
出版信息
Bioorg Med Chem Lett. 2004 Jun 21;14(12):3313-7. doi: 10.1016/j.bmcl.2004.03.063.
In order to find novel nonhydroxamate histone deacetylase (HDAC) inhibitors, a series of thiol-based compounds modeled after suberoylanilide hydroxamic acid (SAHA) was synthesized, and their inhibitory effect on HDACs was evaluated. Compound 6, in which the hydroxamic acid of SAHA was replaced by a thiol, was found to be as potent as SAHA, and optimization of this series led to the identification of HDAC inhibitors more potent than SAHA.
为了寻找新型非异羟肟酸类组蛋白去乙酰化酶（HDAC）抑制剂，合成了一系列以辛二酰苯胺异羟肟酸（SAHA）为模型的含硫醇化合物，并评估了它们对HDAC的抑制作用。发现化合物6（其中SAHA的异羟肟酸被硫醇取代）与SAHA具有同等效力，对该系列化合物的优化导致了比SAHA更有效的HDAC抑制剂的鉴定。
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