Synthesis of cholestane glycosides bearing OSW-1 disaccharide or its 1→4-linked analogue and their antitumor activities

For further structure–activity relationship (SAR) research of OSW saponins, a cholestane glycoside, namely 3β, 16β, 26-trihydroxycholest-5-en-22-one 16-O-(2-O-4-methoxybenzoyl-β-d-xylopyranosyl)-(1→3)-2-O-acetyl-α-l-arabinopyranoside (1) together with two 1→4-linked disaccharide analogues (2 and 3) were synthesized. Their cytotoxic activities were evaluated by the standard MTT assay. Compound 1 showed potent cytotoxicity against five types of human tumor cells, with IC50 ranging between 1.3 and 73 nM.

Graphical abstractThree cholestane glycosides bearing the OSW-1 disaccharide or its 1→4-linked analogue were synthesized, and their cytotoxic activities were determined. Compound 1 showed potent cytotoxicity against five types of human tumor cells, with IC50 ranging between 1.3 and 73 nM.Figure optionsDownload full-size imageDownload as PowerPoint slide