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

- Naturally occurring tigogenin triglycoside 1a and three derivatives 1b-d were prepared via an efficient one-pot sequential glycosylation strategy.
- Partially protected thiogalactosides bearing unprotected 2,4-OH or 4-OH groups were used to significantly simplify the target molecule synthesis.
- CCK-8 assays against HeLa tumor cell indicated that synthetic saponins 1a-d exhibited significantly higher anti-tumor activities than the positive control cisplatin.