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| 苯甲酰胺组蛋白去乙酰化酶抑制剂的合成及抗肿瘤活性 | |
| 引用本文： | 史祥飞,叶清泉,薛阳,赵砚瑾,李庶心.苯甲酰胺组蛋白去乙酰化酶抑制剂的合成及抗肿瘤活性[J].解放军药学学报,2011,27(2):99-102. |
| 作者姓名： | 史祥飞 叶清泉 薛阳 赵砚瑾 李庶心 |
| 作者单位： | 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. 100850 北京,军事医学科学院放射与辐射医学研究所;100048 北京,首都师范大学 |
| 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,HNMR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5a... |
| 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 |
Synthesis and Antitumor Activities of Benzamide Derivatives as Histone Deacetylase Inhibitors |
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| SHI Xiang-fei,YE Qing-quan,XUE Yang,ZHAO Yan-jin,LI Shu-xin.Synthesis and Antitumor Activities of Benzamide Derivatives as Histone Deacetylase Inhibitors[J].Pharmaceutical Journal of Chinese People's Liberation Army,2011,27(2):99-102. | |
| Authors: | SHI Xiang-fei YE Qing-quan XUE Yang ZHAO Yan-jin LI Shu-xin |
| Institution: | 1.Beijing Institute of Radiation Medicine,Beijing 100850,China;2.Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China; 3.Capital Normal University, Beijing 100048, China) |
| Abstract: | 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. |
| Keywords: | cancer histone deaceylase histone deaceylase inhibitors benzamide derivatives |
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