新型蜀羊泉碱衍生物的合成及体外抗肿瘤活性（英文）

Synthesis and in vitro antitumor activities of novel soladulcidine derivatives

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IC ₅₀为（4.8±0.9）μmol/L。
- 蜀羊泉碱衍生物 /
- 合成 /
- 抗肿瘤活性
Abstract: 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 (IC ₅₀=4.8±0.9 μmol/L).
- soladulcidine derivatives /
- synthesis /
- antitumor activity