冬凌草甲素芳胺类衍生物的合成及其抗肿瘤活性  

Synthesis of amino-derivatives of oridonin and their antitumor activity

作　　者：阎学斌[1] 张建业[1] 可钰[2] 周霞[1] 刘宏民[2] 

机构地区：[1]郑州大学化学系,郑州450001 [2]郑州大学药学院,郑州450001

出　　处：《郑州大学学报（医学版）》2007年第1期39-41,共3页Journal of Zhengzhou University(Medical Sciences)

基　　金：国家高技术研究发展计划(863计划)2002AA2Z3242

摘　　要：目的:对冬凌草甲素进行结构改造,合成其芳胺衍生物,并初步评价其抗肿瘤活性。方法:冬凌草甲素分别与4种芳胺发生迈克尔反应,所获产物采用IR、1H-NMR、MS和元素分析确证结构,以冬凌草甲素为阳性对照,采用MTT法观察不同浓度的产物对KB细胞增殖的抑制作用。结果与结论:合成了4个冬凌草甲素的芳胺类衍生物,初步药理试验表明该类化合物对KB细胞株有显著的增殖抑制作用。Aim： To synthesize the aromatic amino-derivatives of oridonin and study their antitumor activity. Methods：The target compounds were synthesized using oridonin and aromatic amines via the Mannich reaction and its antitumor activity against the proliferation of KB cells was observed. Result and conclusion： Four new compounds were obtained and confirmed by spectrum analysis. The obtained compounds have significant antitumor activity against KB cells.

关 键 词：冬凌草甲素 芳胺类衍生物 合成 抗肿瘤活性 

分 类 号：R914.4[医药卫生—药物化学] O621.3[医药卫生—药学]