Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, PR China.
Bioorg Med Chem. 2011 Aug 1;19(15):4437-44. doi: 10.1016/j.bmc.2011.06.046. Epub 2011 Jun 21.
Histone deacetylases (HDACs) are a promising target for treating cancer and some other disorders. Herein, based on the structure of our previously reported tetrahydroisoquinoline-based hydroxamic acids, a novel series of tyrosine-based hydroxamic acid derivatives was designed and synthesized as HDACs inhibitors. Compared with tetrahydroisoquinoline-based hydroxamic acids, tyrosine-based hydroxamic acid derivatives exhibited more potent HDAC8 inhibitory activity. However, the antiproliferative activities and HeLa cell nuclear extract inhibition of several selected tyrosine-based hydroxamic acids were moderate.
组蛋白去乙酰化酶（HDACs）是治疗癌症和一些其他疾病的有前途的靶点。在此，基于我们之前报道的四氢异喹啉基羟肟酸的结构，设计并合成了一系列新型酪氨酸基羟肟酸衍生物作为 HDACs 抑制剂。与四氢异喹啉基羟肟酸相比，酪氨酸基羟肟酸衍生物对 HDAC8 的抑制活性更强。然而，几种选定的酪氨酸基羟肟酸的抗增殖活性和 HeLa 细胞核提取物抑制活性中等。
