Divergent Synthesis of a Pochonin Library Targeting HSP90 and In Vivo Efficacy of an Identified Inhibitor | Zendy

Barluenga Sofia | Zendy; Wang Cuihua | Zendy; Fontaine JeanGonzague | Zendy; Aouadi Kaïss | Zendy; Beebe Kristin | Zendy; Tsutsumi Shinji | Zendy; Neckers Len | Zendy; Winssinger Nicolas | Zendy

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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.

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