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Publication 51  

  1. Divergent Synthesis of a Pochonin Library Targeting HSP90 and In Vivo Efficacy of an Identified Inhibitor
    S. Barluenga, C. Wang, J.-G. Fontaine, K. Aouadi, K. Beebe, S. Tsutsumi, L. Neckers, N. Winssinger
    Angew. Chem. Int. Ed. 2008, 47, 4432-4435

Make a clean breast of it: The generation of a library of pochonin D derivatives by a solid-phase approach has led to the discovery of pochoxime (see scheme), a potent inhibitor of the heat-shock protein 90, with over 100-fold improved incellular activity. Pochoxime was found to be effective in breast tumor xenografts, leading to a reduction in the tumor size.

DOI: 10.1002/anie.200800233 

open archive unige:24735