摘要
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。
Aim To design and synthesize a new series of N-hydroxycinnamamide derivatives and test their activities against histone deacetylases. 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） show potent activities（ IC50 = 2 - 15 μmol· L^-1） and are worthy of further antitumor activity investtgation.
出处
《中国药物化学杂志》
CAS
CSCD
2008年第4期250-253,共4页
Chinese Journal of Medicinal Chemistry
基金
国家高技术研究发展计划项目(863项目
2007AA02Z314)
