Using orthogonal protection–deprotection glycosylation strategy, a series of diosgenyl glycosides with same of monosacchar- ides component but different in sequence were synthesized. The antitumor activity in vitro of synthesized diosgenyl glycosides was evaluated by standard MTT assay. It was observed that diosgenyl glycosides with a rhamnopyranosyl at C20 of glucopyranosyl residue show potent antitumor activity in vitro.
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