Using orthogonal protection-deprotection glycosylation strategy, a series of diosgenyl glycosides with same of monosaccharides 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 C'2 of glucopyranosyl residue show potent antitumor activity in vitro.(C) 2007 Ping Sheng Lei. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.