4-β-硫酯-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成及其抗肿瘤活性  

Synthesis and Antitumor Activity of-4--β-Alkylthiocarbonyl-4-Deoxy-4′ Demethylepipodophyllotoxin

作　　者：陈再新[1] 马维勇[1] 陈秀华[1] 张椿年[1] 

机构地区：[1]上海医药工业研究院,上海200040

出　　处：《中国药物化学杂志》2000年第2期84-87,共4页Chinese Journal of Medicinal Chemistry

摘　　要：为考察 4′ 去甲鬼臼毒素C4位上联结碳原子对活性的影响 ,作者设计并合成C4位 β构型的硫酯取代的衍生物 18个 .这类化合物在体外的抑制L12 10细胞和KB细胞的药理实验中显示出一定的抗肿瘤活性 。Eighteen new 4 β alkylthiocarbonyl 4 deoxy 4′ demethylepipodophyllotoxin were synthesized and screened in vitro against L1210 leukemia and KB cells.Most of them were less active than etoposide.Fatty thioesters have higher activity than aromatic thioesters.The carbon number of the main chain in fatty thioester and the substituent in aromatic thioester don′t affect their activity.

关 键 词：鬼臼毒素 衍生物 抗肿瘤活性 药理 

分 类 号：R914[医药卫生—药物化学]