基于苯并噻吩的异羟肟酸作为高效且选择性的组蛋白去乙酰化酶6（HDAC6）抑制剂的合成。
Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitors.
作者信息
De Vreese Rob, Van Steen Nicholas, Verhaeghe Tom, Desmet Tom, Bougarne Nadia, De Bosscher Karolien, Benoy Veronick, Haeck Wanda, Van Den Bosch Ludo, D'hooghe Matthias
机构信息
SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium.
出版信息
Chem Commun (Camb). 2015 Jun 18;51(48):9868-71. doi: 10.1039/c5cc03295d.
A small library of 3-[(4-hydroxycarbamoylphenyl)aminomethyl]benzothiophenes was prepared and assessed as a novel class of HDAC6 inhibitors, leading to the identification of three representatives as potent and selective HDAC6 inhibitors. Further tests with regard to inflammatory responses indicated that HDAC6 inhibition can be uncoupled from transcriptional inhibition at the level of activated NF-κB, AP-1, and GR.
制备了一个由3-[(4-羟基氨基甲酰基苯基)氨甲基]苯并噻吩组成的小型文库，并将其作为一类新型的组蛋白去乙酰化酶6（HDAC6）抑制剂进行评估，从而鉴定出三种具有强效和选择性的HDAC6抑制剂代表物。关于炎症反应的进一步测试表明，在活化的核因子κB（NF-κB）、活化蛋白-1（AP-1）和糖皮质激素受体（GR）水平上，HDAC6抑制作用可以与转录抑制作用解偶联。
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