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ID: ALA1772946

Journal: Bioorg Med Chem Lett

Title: Identification and initial SAR of silybin: an Hsp90 inhibitor.

Authors: Zhao H, Brandt GE, Galam L, Matts RL, Blagg BS.

Abstract: Through Hsp90-dependent firefly luciferase refolding and Hsp90-dependent heme-regulated eIF2α kinase (HRI) activation assays, silybin was identified as a novel Hsp90 inhibitor. Subsequently, a library of silybin analogues was designed, synthesized and evaluated. Initial SAR studies identified the essential, non-essential and detrimental functionalities on silybin that contribute to Hsp90 inhibition.

CiteXplore: 21273068

DOI: 10.1016/j.bmcl.2010.12.088