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

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Abstract

In order to study the SAR of 5(6)-dihydro-OSW-1, eight 15(α)β-O-glycosyl analogs (2633) 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.

Graphical abstract

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.

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Acknowledgments

Financial support of this research by National Natural Science Foundation of China (NNSFC 30772632) and National Program of New Drug Innovation and Production (2009ZX09301-003) is gratefully acknowledged by authors.

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