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A diversified synthesis of 3-aminosugar analogues of digitoxin and digoxin with potent anticancer activities was explored. The synthesis was based on a highly efficient gold-catalyzed glycosylation reaction with alkynylbenzoate 3-aminoglycosides as glycosyl donors. According to this strategy, a small library containing digitoxin and digoxin analogues with various 3-aminosugar scaffolds was successfully constructed.

Graphical abstract: Gold-catalyzed diversified synthesis of 3-aminosugar analogues of digitoxin and digoxin

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