Enhancement of cyclopamine via conjugation with nonmetabolic sugars.

ABSTRACT: 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.

SUBMITTER: Goff RD 

PROVIDER: S-EPMC3442133 | biostudies-literature | 2012 May

REPOSITORIES: biostudies-literature