Syntheses and Anti-cancer Activities of Glycosylated Derivatives of Diosgenin

In order to obtain better anti-cancer compounds, nine glycosylated derivatives were designed and synthesized using diosgenin as starting material. Their structures were confirmed by H-1 NMR, C-13 NMR and MS spectra. The anti-cancer activities of intermediate compounds 5a-5i and the target compounds 6a-6i were investigated against human leukemia HEL, K562, HL60 and melanoma WM9 cell lines via MTT method. The bioassay results show that these derivatives possess good inhibitory activities against the four cancer cell lines. Furthermore, these derivatives show better inhibitory activities against K562 than against other cell lines, and most derivatives show better inhibitory activities than the parental material. Moreover, compounds 6a-6i are more active than their intermediates 5a-5i when against these cells. The above results demonstrate the effects of glycosylation on 3-OH of diosgenin and acetylation of the sugar moiety on their antitumor activities.