Synthesis and biological evaluation of novel lignan glycosides as anticancer agents.

Novel lignan glycosides 1a-1 h as analogues of cleistanthin A were designed and synthesized. Most of these compounds displayed significant cytotoxicities against four cancer cell lines. Compound 1e displayed better cytotoxicity than cleistanthin A with IC50 values from 1.0 nm to 8.3 nm. Further lysosome acidity assay disclosed that 1e could totally inhibit the activity of V-ATPase at 60 nm.