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Divergent Synthesis of a Pochonin Library Targeting HSP90 and In Vivo Efficacy of an Identified Inhibitor
Author(s) -
Barluenga Sofia,
Wang Cuihua,
Fontaine JeanGonzague,
Aouadi Kaïss,
Beebe Kristin,
Tsutsumi Shinji,
Neckers Len,
Winssinger Nicolas
Publication year - 2008
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200800233
Subject(s) - in vivo , hsp90 inhibitor , hsp90 , chemistry , heat shock protein , cancer research , pharmacology , biochemistry , medicine , biology , microbiology and biotechnology , gene
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.