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Targeting the Hsp90 chaperone: synthesis of novel resorcylic acid macrolactone inhibitors of Hsp90.

Authors
Type
Published Article
Journal
Chemistry - A European Journal
1521-3765
Publisher
Wiley Blackwell (John Wiley & Sons)
Publication Date
Volume
16
Issue
9
Pages
2758–2763
Identifiers
DOI: 10.1002/chem.200902766
PMID: 20087915
Source
Medline
License
Unknown

Abstract

A series of benzo-macrolactones has been prepared by chemical synthesis, and evaluated as inhibitors of heat shock protein 90 (Hsp90), an emerging attractive target for novel cancer therapeutic agents. A new synthesis of these resorcylic acid macrolactone analogues of the natural product radicicol is described in which the key steps are the acylation and ring opening of a homophthalic anhydride to give an isocoumarin, followed by a ring-closing metathesis to form the macrocycle. The methodology has been extended to a novel series of macrolactones incorporating a 1,2,3-triazole ring.

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