Enhancement of Cyclopamine via Conjugation with Nonmetabolic Sugars

作者: Randal D. Goff , Jon S. Thorson

DOI: 10.1021/OL300703Z

关键词:

摘要: The Veratrum alkaloid cyclopamine, an inhibitor of cancer stem cell growth, was used as a representative scaffold to evaluate the inhibitory impact glycosylation with group nonmetabolic saccharides, such d-threose. In five-step divergent process, 32-member glycoside library created and assayed determine that glycosides sugars notably improved GI50 value cyclopamine while metabolic sugars, d-glucose, did not.

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