Department of Chemistry, University of West Florida , 11000 University Parkway, Pensacola, Florida 32514, United States, and Center for Pharmaceutical Research and Innovation, University of Kentucky College of Pharmacy , 789 South Limestone Street, Lexington, Kentucky 40536-0596, United States.
Org Lett. 2012 May 18;14(10):2454-7. doi: 10.1021/ol300703z. Epub 2012 Apr 27.
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 GI50 value of cyclopamine while metabolic sugars, such as d-glucose, did not.
白屈菜碱是一种抑制癌症干细胞生长的生物堿，被用作代表性支架，以评估一组非代谢糖，如 d-苏糖，对其进行糖基化的抑制作用。在一个五步发散过程中，创建了一个 32 成员的糖苷文库并进行了检测，结果表明，这些糖的糖苷显著提高了白屈菜堿的 GI50 值，而代谢糖，如 d-葡萄糖，则没有。
