苯甲酰胺类组蛋白去乙酰化酶抑制剂的合成及其抗肿瘤活性研究  

Synthesis and Biological Evaluation of Benzamides as Histone Deacetylase Inhibitors

作　　者：张志杰[1,2] 赵砚瑾[2] 刘意林 江发龙[2] 姚郑林[2] 匡先照[2] 李庶心[1,2] 

机构地区：[1]安徽医科大学,合肥230032 [2]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《科学技术与工程》2015年第13期133-136,148,共5页Science Technology and Engineering

基　　金：国家自然科学基金(30772628)资助

摘　　要：以MS-275为先导化合物,设计并合成8个苯甲酰胺类组蛋白去乙酰化酶抑制剂,其结构经MS与1H-NMR确证。以MS-275为阳性对照药物,测试8个目标化合物对人乳腺癌细胞MCF-7和人肺癌细胞A549的体外抗肿瘤细胞增殖活性,结果显示,合成的8个目标化合物中有6个化合物表现出较好的抑制肿瘤的活性,尤其是化合物5a与7b对肿瘤细胞的体外抑制活性与MS-275相比有较为显著地提高,可为进一步研究提供参考。MS-275 was taken as the lead compound, eight benzamides as histone deacetylase inhibitor were de- signed and synthesized, and their structures were identified by MS and ^1H-NMR. A test of target compounds on hu- man breast cancer ceils MCF-7 and human lung cancer cells A549 in vitro antiproliferative activity has been done, in which MS-275 was taken as a positive control. The results showed that six compounds of target compounds showed better tumor suppression activity, especially the vitro inhibitory activity on tumor cells of compounds 5a and 7b has a more remarkably improved compared with the MS-275,they can be mentioned for further study as reference.

关 键 词：苯甲酰胺类 组蛋白去乙酰化酶抑制剂 合成 抗肿瘤 

分 类 号：R914.5[医药卫生—药物化学]