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).