Synthesis and Evaluation of the alpha-D-/alpha-L-Rhamnosyl and Amicetosyl Digitoxigenin Oligomers as Antitumor Agents

[摘要]：A highly regio- and stereoselective asymmetric synthesis of rhamnosyl- and amicetpsyl-digitoxigenin analogues has been established via palladium catalyzed glycosylation followed by big-/tris-dihydroxylation or bis-/tris-diimide reduction. The alpha-L-rhamnose and alpha-L-amicetose digitoxin monosaccharide analogues displayed stronger apoptosis inducing activity and cytotoxicity against nonsmall cell human lung cancer cells (NCI-H460) than its D-diastereomeric isomers in a sugar chain length dependent manner.

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