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Department of Oncology, Faculty of Medicine and Dentistry, University of Alberta, 11560 University Ave, Edmonton AB T6G 1Z2, Canada
; Fax: +1 780 432 8483
; Tel: +1 780 989 8150
Department of Cell Biology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton AB T6G 2H7, Canada
; Fax: +1 780 492 0450
; Tel: +1 780 492 1804
Org. Biomol. Chem., 2012,10, 6724-6731
18 Apr 2012,
06 Jul 2012
First published online
06 Jul 2012
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.
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Organic & Biomolecular Chemistry
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