摘要
蜀羊泉碱是一类来源于白英的甾体生物碱,具有多种生物活性。本文通过对其C-3位羟基、E环和F环进行结构修饰,合成了10个蜀羊泉碱衍生物,并对人前列腺癌细胞PC-3进行了体外癌细胞增殖抑制实验。体外实验显示部分化合物对人前列腺癌细胞PC-3有较好增殖抑制作用,其中化合物19活性最好,其IC50为(4.8±0.9)μmol/L。
Soladulcidine is a steroidal alkaloid abundant in Solanum dulcamara L.with antitumor and other biological activities.In this study,ten soladulcidine derivatives were synthesized through esterification at C-3-hydroxy group,modification at NH group of F ring or esterification of E ring-opening products.The in vitro antiproliferative activity of these synthesized derivatives against prostate cancer（PC-3） cell line was assessed.Within this series of compounds,compound 19 exhibited the most potent inhibitory effect against the proliferation of PC-3 cell line（IC50=4.8±0.9μmol/L）.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2010年第6期493-498,共6页
Journal of China Pharmaceutical University
关键词
蜀羊泉碱衍生物
合成
抗肿瘤活性
soladulcidine derivatives
synthesis
antitumor activity
