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Issue 33, 2012
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Fluorine- and rhenium-containing geldanamycin derivatives as leads for the development of molecular probes for imaging Hsp90

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Abstract

Heat shock protein 90 (Hsp90) is an ATP-dependent molecular chaperone responsible for protein quality control in cells. Hsp90 has been shown to be overexpressed in many human cancers. This has prompted extensive research on Hsp90 inhibitors as novel anticancer agents and, more recently, the development of molecular probes for imaging Hsp90 expression in vivo. This work describes the development of various fluorine-containing and rhenium-containing geldanamycin derivatives as leads for the development of corresponding 18F-labeled and 99mTc-labeled PET and SPECT probes for molecular imaging of Hsp90 expression. All compounds were evaluated in an in vitro ATPase activity assay using Hsp90 isoform Hsp82p. Fluorobenzoylated geldanamycin derivative 5 displayed comparable inhibitory potency like parent compound geldanamycin.

Graphical abstract: Fluorine- and rhenium-containing geldanamycin derivatives as leads for the development of molecular probes for imaging Hsp90

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Article information


Submitted
18 Apr 2012
Accepted
06 Jul 2012
First published
06 Jul 2012

Org. Biomol. Chem., 2012,10, 6724-6731
Article type
Paper

Fluorine- and rhenium-containing geldanamycin derivatives as leads for the development of molecular probes for imaging Hsp90

F. Wuest, V. Bouvet, B. Mai and P. LaPointe, Org. Biomol. Chem., 2012, 10, 6724
DOI: 10.1039/C2OB25744K

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