苯甲酰胺组蛋白去乙酰化酶抑制剂的合成及抗肿瘤活性  

Synthesis and Antitumor Activities of Benzamide Derivatives as Histone Deacetylase Inhibitors

作　　者：史祥飞[1] 叶清泉[2] 薛阳[1] 赵砚瑾[1] 李庶心[1,3] 

机构地区：[1]军事医学科学院放射与辐射医学研究所,北京100850 [2]江西中医学院,江西南昌330006 [3]首都师范大学,北京100048

出　　处：《解放军药学学报》2011年第2期99-102,共4页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金：国家自然科学基金;No.30772628

摘　　要：目的设计合成苯甲酰胺嘧啶衍生物,并初步评价其抗肿瘤活性。方法以4-氨甲基苯甲酸为原料经过4步反应,合成了12个苯甲酰胺衍生物,结构经过1H NMR和MS鉴定,采用MTT法筛选了目标化合物的抗肿瘤活性并进行初步评价。结果合成了12个目标化合物,均未见文献报道。5个化合物显示较好的肿瘤细胞增殖抑制活性。结论化合物5 a、5b、5 c、5 e、5 j显示较好的体外抗肿瘤活性,值得进一步研究。Objective To synthesize novel benzamide derivatives as antitumor drug candidates.Methods Twelve derivatives of benzamide were synthesized in four steps from 4-（aminomethyl）benzoic acid.Their structures were identified by 1H-NMR and MS.The antitumor activities of the compounds were screened by MTT methods.Results Twelve novel compounds were synthesized.Five compounds inhibited the proliferation of several human cancer cell lines.Conclusion Compounds（5a、5b、5c、5e、5j） have better antitumor activities and are worthy of further studies.

关 键 词：肿瘤 组蛋白去乙酰化酶 组蛋白去乙酰化酶抑制剂 苯甲酰胺衍生物 

分 类 号：R915.5[医药卫生—微生物与生化药学]