Document Report Card

ID: ALA2057099

Journal: J Med Chem

Title: Synthesis of rocaglamide hydroxamates and related compounds as eukaryotic translation inhibitors: synthetic and biological studies.

Authors: Rodrigo CM, Cencic R, Roche SP, Pelletier J, Porco JA.

Abstract: The rocaglates/rocaglamides are a class of natural products known to display potent anticancer activity. One such derivative, silvestrol, has shown activity comparable to taxol in certain settings. Here, we report the synthesis of various rocaglamide analogues and identification of a hydroxamate derivative (-)-9 having activity similar to silvestrol in vitro and ex vivo for inhibition of protein synthesis. We also show that (-)-9 synergizes with doxorubicin in vivo to reduce Eμ-Myc driven lymphomas.

CiteXplore: 22128783

DOI: 10.1021/jm201263k