Technetium glucose complexes as potential cancer imaging agents

Bioorganic & Medicinal Chemistry Letters
Rosina DapuetoWilliams Porcal

Abstract

GLUT's (facilitative glucose transporters) over-expression in tumor cells has allowed the detection of several cancer types, using a glucose analogue ((18)F-FDG) with PET images, worldwide. New glucose analogs radiolabeled with (99m)Tc could be a less-expensive and more accessible alternative for diagnosis using SPECT imaging. d-Glucose ((99m)Tc-IDAG) and 2-d-deoxyglucose ((99m)Tc-AADG) organometallic complexes were proposed and studied as potential (18)F-FDG surrogates. The glucose complexes were prepared and evaluated as potential cancer imaging agents, in a melanoma tumor model. Iminodiacetic acid (IDA) and aminoacetate (AA) moieties were chosen as chelating system for radiolabeling with (99m)Tc. Tumor uptake of the formed complexes was evaluated in B16 murine cell line in vitro and in vivo in melanoma bearing C57BL/6 mice. In vitro and in vivo studies were conducted with (18)F-FDG in order to compare the uptake of (99m)Tc-glucose complexes in the tumor model. IDAG and AADG compounds were synthesized and radiolabeled with (99m)TcO4(-) to obtain the (99m)Tc-IDAG and (99m)Tc-AADG complexes in high yield and stability. In vitro cell studies showed maximum uptake at 60 min for complexes, (99m)Tc-IDAG and (99m)Tc-AADG, with 6% an...Continue Reading

References

Nov 2, 2004·Nature Reviews. Cancer·Robert A Gatenby, Robert J Gillies
Jun 3, 2005·Nature Reviews. Drug Discovery·Danielle H Dube, Carolyn R Bertozzi

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Citations

Jun 13, 2017·Chemical Reviews·Bagher Eftekhari-Sis, Maryam Zirak
Dec 1, 2015·Nuclear Medicine Communications·Renata S FernandesAndré L B de Barros

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