臼毒素类衍生物的合成及生物活性  

Synthesis of podophyllotoxin derivatives as anti-cancer agents and its activity

作　　者：陈静[1,2] 孙有光[1] 白淑芳[2] 毕文超[2] 谢文利[2] 肖斌[2] 王薇薇[2] 陈虹[2] 

机构地区：[1]天津理工大学化学化工学院,天津300384 [2]天津武警医学院生药教研室,天津300162

出　　处：《天津理工大学学报》2009年第2期22-25,共4页Journal of Tianjin University of Technology

基　　金：天津市自然科学基金(06YFJ2JCO2700;08JCYBJC070000)

摘　　要：为了寻找活性高、抗肿瘤多药耐药好的新药物改善肿瘤的化疗效果,本文设计将鬼臼毒素内酯环用水合肼打开,然后与不同的醛类相结合,生成9个新的未见报道的鬼臼酰腙类衍生物.经MTT法测定此类衍生物的抗宫颈癌细胞、胃癌细胞的抑制作用,发现大部分都具有较好的抗肿瘤活性.而且,对耐药细胞KBV200测定发现,其中3个化合物3e,3g和3i具有良好的抗多药耐药性.The purpose of this study is to find out active and efficient drug resistance modulators for improving the efficacy of chemotherapy. A new series of podophyllotoxin derivatives with the D-ring lactone opened were synthesized in two steps from podophyllotoxin and evaluated as antitumur agents in vitro. Most of the derivatives exhibit antitumur activity. The conpounds 3e, 3g and 3i, synthesized from o-chloricbenzoic aldehyde, p-hydroxybenzoic aldehyde and dibrombenzoic aldehyde, can overcome MDR well.

关 键 词：鬼臼毒素衍生物 内酯环 合成 抗癌活性 多药耐药性 

分 类 号：R979.1[医药卫生—药品]