一组新的N-羟基肉桂酰胺类组蛋白去乙酰化酶抑制剂的合成和初步活性研究

目的设计合成了一组新的N-羟基肉桂酰胺类衍生物并测定其对组蛋白去乙酰化酶（HDACs）的抑制活性。方法以阿魏酸为原料，经酯化、Williamson反应、皂化、缩合4步反应合成了一组新的N-羟基肉桂酰胺类衍生物；用组蛋白去乙酰化酶活性检测试剂盒测定该组化合物体外抑酶活性。结果与结论合成了11个未见文献报道的N一羟基肉桂酰胺类衍生物，其结构经过。H-NMR、MS、和IR确认。其中化合物5a、5b、5e和5k的体外抑酶活性较强（IC50=2--15 μmol·L^-1），有可能具有抗肿瘤活性，值得进一步研究。

Synthesis and activities study of a new series of histone deacetylases(HDACs) inhibitors of N-hydroxycinnamamide derivatives

Abstracts: Aim To design and synthesize a new series of N-hydroxycinnamamide derivatives and test their activities against histone deacetylases(HDACs). Methods The target compounds were synthesized through esterification, Williamson reaction, saponification and condensation from ferulic acid and their activities were tested in vitro with an HDACs activity assay kit. Results and conclusion Eleven novel N-hydroxycinnamamide derivatives were synthesized and their structures were comfirmed by 1H-NMR, MS and IR. Four compounds(5a、5b、5e and 5k) showed potent activities(IC50=2-15 μmol.L-1) and are worthy of further antitumor activity investigation.