Efficient one-pot synthesis of tigogenin saponins and their antitumor activities

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• 作者：Guofeng Gu ; Lian An ; Min Fang ; Zhongwu Guo
• 关键词：Saponin ; One-pot sequential glycosylation ; Thioglycoside ; Antitumor activity
• 刊名：Carbohydrate Research
• 出版年：13 January, 2014
• 年：2014
• 卷：383
• 期：Complete
• 页码：21-26
• 全文大小：624 K

文摘

An efficient synthesis of naturally occurring tigogenin triglycoside 1a and its three derivatives 1b-d bearing different carbohydrate moieties, as well as their antitumor activities, is described. Partially protected thiogalactosides bearing unprotected 2,4-OH or 4-OH groups were used to facilitate regioselective reactions for one-pot sequential multi-step glycosylation, which has significantly simplified the target molecule synthesis. The synthetic saponins 1a-d exhibited much higher anti-tumor activities than the positive control cisplatin against the human epithelial cervical cancer cell (HeLa) as evaluated by CCK-8 assay.