Abstract: Fifteen novel diosgenin derivatives were designed and synthesized.The structures of all derivatives were confirmed by ¹HNMR, ¹³C NMR, IR and HR-MS spectra. The antitumor activities of the fifteen derivatives were evaluated against A431, H1975 cell lines by MTT assay. The preliminary bioassay test suggested that most of these diosgenin derivatives showed different degrees of activities.

Key words: diosgenin, structural modification, acylation reaction, antitumor activity, amide derivatives