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

Barluenga, Sofia; Wang, Cuihua; Fontaine, Jean-Gonzague; Aouadi, Kaïss; Beebe, Kristin; Tsutsumi, Shinji; Neckers, Len; Winssinger, Nicolas

doi:10.1002/anie.200800233

Scientific article

English

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

Contributors

Barluenga, Sofia; Wang, Cuihua; Fontaine, Jean-Gonzague; Aouadi, Kaïss; Beebe, Kristin; Tsutsumi, Shinji; Neckers, Len; Winssinger, Nicolas

Published in

Angewandte Chemie, vol. 47, no. 23, p. 4432-4435

Publication date

2008

Abstract

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.

Keywords

antitumor agents
bioorganic chemistry
natural products
solid-phase synthesis
synthesis design

UNIGE affiliation entities

Not a UNIGE publication

Citation (ISO format)

BARLUENGA, Sofia et al. Divergent Synthesis of a Pochonin Library Targeting HSP90 and In Vivo Efficacy of an Identified Inhibitor. In: Angewandte Chemie, 2008, vol. 47, n° 23, p. 4432–4435. doi: 10.1002/anie.200800233

Article (Published version)

Identifiers

PID : unige:24735
DOI : 10.1002/anie.200800233

Journal ISSN

1433-7851

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12/12/2012 09:01:00

First validation

12/12/2012 09:01:00

Update

13/10/2025 23:52:32

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01/07/2026 06:10:02