水溶性大黄素衍生物的合成及抗白血病的初步研究  

Synthesis of soluble emodin derivatives and their properties of anti-leukemia

作　　者：邱炳林[1] 李静[2] 陈彩[2] 陈英玉[2] 胡建达[2] 袁耀锋[1] 王文峰[1] 

机构地区：[1]福州大学化学化工学院,福建福州350108 [2]福建医科大学附属协和医院,福建省血液病研究所,福建福州350001

出　　处：《中国药物化学杂志》2010年第5期353-357,共5页Chinese Journal of Medicinal Chemistry

基　　金：福建省青年人才基金资助项目(2007F3048);福州大学科技发展基金资助项目(2008-XQ-11);福建省高校新世纪优秀人才计划项目(NCETFJ-0604);福建医科大学教授基金

摘　　要：目的改善大黄素衍生物的水溶性问题,以期得到一些抗白血病活性较好的大黄素衍生物。方法以大黄素为原料,经过羟基保护、N-溴代丁二酰亚胺(NBS)参与的溴代反应、与叔胺成盐反应制得目标化合物。结果与结论合成了11个未见文献报道的大黄素衍生物,其结构经IR、1H-HNMR谱和元素分析确证。化合物3h、3i和3j对白血病细胞K562和Jurkat细胞株有较好的活性。Aim To synthesize some emodin derivatives with anti-leukemia properties and to increase their water-solubility.Methods Eleven compounds were prepared from emodin through the hydroxyl protection,bromination with NBS and then reaction with a series of tertiary amines.Results and conclusion Eleven new compounds were synthesized and their structures were characterized by IR,1H-NMR and elemental analysis.Compounds 3h,3i,and 3j have good inhibitory activity on the K562 and Jurkat leukemia cells.

关 键 词：大黄素 衍生物 白血病 水溶性 MTT法 

分 类 号：R284.1[医药卫生—中药学] R733.7[医药卫生—中医学]