Modifying the glycosidic linkage in digitoxin analogs provides selective cytotoxins.
نویسندگان
چکیده
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.
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عنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 18 2 شماره
صفحات -
تاریخ انتشار 2008