Carbohydrate conjugates for molecular imaging and radiotherapy: 99mTc(I) and 186Re(I) tricarbonyl complexes of N-(2'-Hydroxybenzyl)-2-amino-2-deoxy-D-glucose

Bioconjug Chem. 2004 Jul-Aug;15(4):923-6. doi: 10.1021/bc0499681.

Abstract

An approach to a new class of potential radiopharmaceuticals is demonstrated by the labeling of a glucosamine derivative with the tricarbonyls of 99mTc and 186Re. 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)3Br3] to form the neutral complex [(L2)Re(CO)3] in 40% yield. 1H and 13C 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 [99mTc(CO)3(H2O)3]+ and [186Re(CO)3(H2O)3]+ was achieved in aqueous conditions in 95 +/- 2% and 94 +/- 3% average radiochemical yields, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Carbohydrates / chemistry*
  • Chromatography, High Pressure Liquid
  • Glucosamine / analogs & derivatives*
  • Glucosamine / chemical synthesis
  • Glucosamine / chemistry*
  • Magnetic Resonance Imaging / instrumentation*
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Radioisotopes
  • Radiopharmaceuticals / chemistry*
  • Rhenium / chemistry*
  • Rhenium / therapeutic use
  • Technetium Compounds / chemical synthesis
  • Technetium Compounds / chemistry*
  • Technetium Compounds / therapeutic use

Substances

  • Carbohydrates
  • N-(2'-hydroxybenzyl)-2-amino-2-deoxyglucose
  • Radioisotopes
  • Radiopharmaceuticals
  • Technetium Compounds
  • Rhenium
  • Glucosamine