Octadentate oxine-armed bispidine ligand for radiopharmaceutical chemistry
In this study, we present the synthesis and characterization of the octadentate bispidine ligand, H2bispox2 and its complexes with medicinally useful radiometal nuclides (111In3+ and 177Lu3+), including their X-ray diffraction single crystal structures with the stable isotopes. 111InCl3 radiolabels...
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| Main Authors: | , , , , , , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
2019
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| In: |
Inorganic chemistry
Year: 2019, Volume: 58, Issue: 13, Pages: 8685-8693 |
| ISSN: | 1520-510X |
| DOI: | 10.1021/acs.inorgchem.9b01016 |
| Online Access: | Verlag, Volltext: https://doi.org/10.1021/acs.inorgchem.9b01016
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| Author Notes: | Neha Choudhary, Alexander Dimmling, Xiaozhu Wang, Lily Southcott, Valery Radchenko, Brian O. Patrick, Peter Comba, Chris Orvig |
| Summary: | In this study, we present the synthesis and characterization of the octadentate bispidine ligand, H2bispox2 and its complexes with medicinally useful radiometal nuclides (111In3+ and 177Lu3+), including their X-ray diffraction single crystal structures with the stable isotopes. 111InCl3 radiolabels the ligand quantitatively at ambient conditions ([L] = 10-5 M, room temperature, pH 7 and 15 min) and the in vitro human serum stability assays demonstrated high stability of the [111In(bispox2)]+ complex over 5 days. Moreover, the β- emitter 177Lu radiolabels the ligand at 37 °C in 30 min (pH 8). These initial investigations reveal the potential of the octadentate bispidine ligand H2bispox2 as a useful chelator for 111In and 177Lu-based radiopharmaceuticals. |
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| Item Description: | Gesehen am 10.10.2019 |
| Physical Description: | Online Resource |
| ISSN: | 1520-510X |
| DOI: | 10.1021/acs.inorgchem.9b01016 |