背景：组蛋白去乙酰化酶（HDACs）在转录和表达的表观遗传调控中扮演着重要角色。HDAC1过表达在许多癌症中出现。方法学：作者合成并评估了27个新的香豆素偶氮酰胺衍生物的HDAC1抑制活性。这些化合物在美国国家癌症研究所进行了筛选，并选择了5k和5u进行五剂量实验。化合物5k对MOLT-4和LOX-IMVI显示出GI50值分别为0.294和0.264 μM，而5u分别为0.189和0.263 μM。这两个衍生物的活性均优于entinostat和suberoylanilide hydroxamic acid。化合物5k在ACHN细胞上的IC50值为1.00 μM。结论：香豆素衍生物表现出有希望的HDAC1抑制潜力，并值得作为抗癌剂进行进一步开发。

Background: Histone deacetylases (HDACs) play a vital role in the epigenetic regulation of transcription and expression. HDAC1 overexpression is seen in many cancers. Methodology: The authors synthesized and evaluated 27 novel coumarin-based amide derivatives for HDAC1 inhibitory activity. The compounds were screened at the US National Cancer Institute, and 5k and 5u were selected for five-dose assays. Compound 5k showed GI50 values of 0.294 and 0.264 μM against MOLT-4 and LOX-IMVI, whereas 5u had GI50 values of 0.189 and 0.263 μM, respectively. Both derivatives showed better activity than entinostat and suberoylanilide hydroxamic acid. Compound 5k exhibited an IC50 value of 1.00 μM on ACHN cells. Conclusion: Coumarin derivatives exhibited promising HDAC1 inhibitory potential and warrant future development as anticancer agents.