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Enhancement of Cyclopamine via Conjugation with Nonmetabolic Sugars

  作者 GOFF RANDAL D; THORSON JON S  
  选自 期刊  Organic Letters;  卷期  2012年14-10;  页码  2454-2457  
  关联知识点  
 

[摘要]The Veratrum alkaloid cyclopamine, an inhibitor of cancer stem cell growth, was used as a representative scaffold to evaluate the inhibitory impact of glycosylation with a group of nonmetabolic saccharides, such as D-threose. In a five-step divergent process, a 32-member glycoside library was created and assayed to determine that glycosides of such sugars notably improved the GI(50) value of cyclopamine while metabolic sugars, such as D-glucose, did not.

 
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