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Carbohydrate conjugates for molecular imaging and radiotherapy: Tc-99m(I) and Re-186(I) tricarbonyl complexes of N-(2 ’-hydroxybenzyl)-2-amino-2-deoxy-D-glucose

TitleCarbohydrate conjugates for molecular imaging and radiotherapy: Tc-99m(I) and Re-186(I) tricarbonyl complexes of N-(2 ’-hydroxybenzyl)-2-amino-2-deoxy-D-glucose
Publication TypeJournal Article
Year of Publication2004
AuthorsBayly, SR, Fisher, CL, Storr, T, Adam, MJ, Orvig, C
JournalBioconjugate Chemistry
Volume15
Pagination923-926
Date PublishedJul-Aug
Type of ArticleArticle
ISBN Number1043-1802
KeywordsBIOMOLECULES, GLUCOSE, LIGAND SYSTEMS, RADIOPHARMACEUTICALS, SUGARS
Abstract

An approach to a new class of potential radiopharmaceuticals is demonstrated by the labeling of a glucosamine derivative with the tricarbonyls of Tc-99m and Re-186. The proligand HL2 (N-(2’-hydroxybenzyl)-2-amino-2-deoxy-d-glucose) was produced by hydrogenation of the corresponding Schiff base and reacted with [NEt4](2)[Re(CO)(3)Br-3] to form the neutral complex [(L-2)Re(CO)(3)] in 40% yield. H-1 and C-13 NMR spectra indicate that the {Re(CO)(3)} core is bound in a tridentate fashion via the amino N, phenolato O, and C-3 hydroxyl O atoms of the ligand. At the tracer-level, labeling of HL2 with [Tc-99m(CO)(3)(H2O)(3)](+) and [Re-186(CO)(3)(H2O)(3)](+) was achieved in aqueous conditions in 95 +/- 2% and 94 +/- 3% average radiochemical yields, respectively.

URL<Go to ISI>://000222880900032