4'-去甲基表鬼臼毒素酯类衍生物的合成及初步抗肿瘤活性  

Synthesis and in vitro Antitumor Activity of 4'-Demethylepipodophyllotoxin Carboxylic Ester Derivatives

作　　者：李湘[1] 肖旭华[1] 姚利霞[1] 孙亚飞[1] 沈舜义[1] 

机构地区：[1]中国医药工业研究总院上海医药工业研究院生物制药部,上海201203

出　　处：《中国医药工业杂志》2017年第9期1287-1292,共6页Chinese Journal of Pharmaceuticals

摘　　要：为寻找高效低毒且作用谱广的鬼臼毒素类抗肿瘤药物,以4'-去甲基表鬼臼毒素为起始原料,用不同结构的芳香羧酸对其进行修饰,设计合成了17个4'-去甲基表鬼臼毒素酯类新化合物,通过1H NMR和ESI-MS确证其结构,并采用MTT法评价了目标化合物对人肝癌(HepG2)、人肺癌(A549)、人口腔癌(KB)及小鼠白血病细胞(L1210)的抑制活性。结果表明,大多数化合物对肿瘤细胞均表现出较好的抑制作用。In order to find novel epipodophyllotoxins antitumor drugs, seventeen 4＇-demethylepipodophyllo- toxin carboxylic ester compounds were synthesized from 4＇-demethylepipodophyllotoxin via condensation with some aromatic carboxylic acids. All of them have been characterized by ^1H NMR and ESI-MS, and the effect of the synthesized compounds against proliferation ofA549, HepG2, KB, L1210 cells were evaluated by MTT test. Most of these compounds showed moderate inhibitory activities.

关 键 词：4'-去甲基表鬼臼毒素 肿瘤 抑制活性 合成 

分 类 号：R914[医药卫生—药物化学]