期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 9, 期 4, 页码 1071-1078出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c0ob00504e
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The development of molecular imaging agents with multiple functions has become a major trend in radiopharmaceutical chemistry. We present herein the syntheses of trifunctional compounds, combining an acridine orange (AO) based intercalator with a GRP receptor specific bombesin like peptide (BBN). Metal-mediated conjugation of these two functions via the [2 + 1] approach to the third function, the [M(CO)(3)](+) (M = Tc-99m, Re) moiety, yielded the final trifunctional molecules. The strongly fluorescent acridine orange, a nuclear targeting agent, has been derivatised with 4-imidazolecarboxylate as a bidentate ligand and bombesin with an isonitrile group as a monodentate ligand. For cell and nuclear uptake studies, [Re(L-1-BBN)(L-2-Ical)(CO)(3)] type complexes were synthesized and characterized. For radiopharmaceutical purposes, the Tc-99m analogues have been prepared in a stepwise synthesis. Fluorescence microscopy studies on PC-3 cells, bearing the BBN receptor, showed high and rapid uptake into the cytoplasm. For the bifunctional molecule, lacking the BBN peptide, no internalization was observed.
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