Design and synthesis of a tetrahydroisoquinoline-based hydroxamate derivative (ZYJ-34v), an oral active histone deacetylase inhibitor with potent antitumor activity.
Design and synthesis of a tetrahydroisoquinoline-based hydroxamate derivative (ZYJ-34v), an oral active histone deacetylase inhibitor with potent antitumor activity.
复制标题
设计和合成基于四氢异喹啉的异羟肟酸酯衍生物（ZYJ-34v），一种具有有效抗肿瘤活性的口服活性组蛋白脱乙酰酶抑制剂。
DOI：
10.1111/cbdd.12144
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发表时间：
2013
影响因子：
3
通讯作者：
Xu,Wenfang
中科院分区：
文献类型：
--
作者：
Zhang,Yingjie;Liu,Chunxi;Chou,CJames;Wang,Xuejian;Jia,Yuping;Xu,Wenfang
In our previous study, we developed a novel series of tetrahydroisoquinoline‐based hydroxamic acid derivatives as histone deacetylase inhibitors (Bioorg Med Chem, 2010, 18, 1761–1772;J Med Chem, 2011, 54, 2823–2838), among which, compound ZYJ‐34c (1) was identified and validated as the most potent one with markedin vitroandin vivoantitumor potency (J Med Chem, 2011, 54, 5532–5539.). Herein, further modification in1afforded another oral active analog ZYJ‐34v (2) with simplified structure and lower molecular weight. Biological evaluation of compound2showed efficacious inhibition against histone deacetylase 1, 2, 3, and 6, which was confirmed by Western blot analysis results. Most importantly, compound2exhibited similar even more potentin vitroandin vivoantitumor activities relative to the approved histone deacetylase inhibitor SAHA.
