Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365390 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
A chemoselective reaction between oxyamines and unprotected, unactivated reducing sugars was used to construct for the first time a panel of linkage-diversified neoglycosides. This panel of digitoxin analogs included potent and selective tumor cytotoxins; cytotoxicity was dependent on the structure of the glycosidic linkage. These results validate linkage diversification through neoglycosylation as a unique and simple strategy to powerfully complement existing methods for the optimization of glycoconjugates.
Graphical abstractFor the first time a panel of linkage-diversified neoglycosides was constructed. This panel of digitoxin analogs included potent and selective tumor cytotoxins; cytotoxicity was dependent on the structure of the glycosidic linkage.Figure optionsDownload full-size imageDownload as PowerPoint slide