Investigation of Hsp90 Structure-Activity Relationships in Epigallocatechin Gallate

(-)-Epigallocatechin gallate (EGCG) is a polyphenolic natural product that inhibits the key chaperone protein Hsp90 by binding to the carboxy terminal portion of the protein. The natural product has modest activity as an Hsp90 inhibitor and there is little information in the literature on structure activity relationships for EGCG analogs. Previous studies from this laboratory provided initial data on the effect of a limited range of changes associated with functional groups, substituents and stereochemistry. The focus of this research is to explore these initial results in more detail with a focus on the synthesis of EGCG analogs with more drug like features