合成组蛋白去乙酰化酶（HDACs）羟肟酸抑制剂的 N'-丙基酰肼类似物，并评估它们对 HDACs 活性和丙型肝炎病毒（HCV）复制的影响。
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).
机构信息
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilova 32, Moscow 119991, Russia.
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilova 32, Moscow 119991, Russia.
出版信息
Bioorg Med Chem Lett. 2019 Aug 15;29(16):2369-2374. doi: 10.1016/j.bmcl.2019.06.006. Epub 2019 Jun 5.
N'-Propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs), including tubastatin A, vorinostat and belinostat, were synthesized. All prepared compounds inhibited HDAC1/2/3, but not HDAC6, except for one hydrazide analog of HDAC4/5/7 inhibitor that was completely inactive. A novel 4-substituted derivative of N'-propylbenzohydrazide with extremely high anti-HCV activity was discovered.
合成了组蛋白去乙酰化酶（HDACs）的羟肟酸抑制剂 N'-丙基酰肼类似物，包括曲古抑菌素 A、伏立诺他和贝利司他。所有合成的化合物均抑制 HDAC1/2/3，但不抑制 HDAC6，除了一个 HDAC4/5/7 抑制剂的酰肼类似物完全没有活性。发现了一种新型的 N'-丙基苯甲酰肼 4-取代衍生物，具有极高的抗 HCV 活性。
Zotero 插件