Synthesis of 5(6)-dihydro-OSW-1 analogs bearing three kinds of disaccharides linking at 15-hydroxy and their antitumor activities

In order to study the SAR of 5(6)-dihydro-OSW-1, eight 15(α)β-O-glycosyl analogs (26–33) carrying three kinds of disaccharides including [β-d-Xylp-(1–3)-α-l-Arap], [β-d-Xylp-(1–4)-α-l-Arap] and [α-l-Rhap-(1–2)-(α)β-d-Glcp] were designed and synthesized. Their in vitro antitumor activities were tested by the standard MTT assay which disclosed that compound 33 (IC50 = 0.28–0.52 μM) showed potential antitumor activities.

Eight 15(α)β-O-glycosyl 5(6)-dihydro-OSW-1 analogs bearing three kinds of disaccharide side chains were synthesized and evaluated for their antitumor activities.Figure optionsDownload as PowerPoint slide