Synthesis of Bispidine-Based Prostate-Specific Membrane Antigen-Targeted Conjugate and Initial Investigations
Nowadays, PSMA ligands are widely used for radiotheragnostic purposes in prostate cancer. The synthesis of a PSMA-Bisp conjugate was developed and realized with good yield (overall yield ~58% for the last two steps). All newly synthesized compounds were characterized by physicochemical methods: <...
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| Main Authors: | , , , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-02-01
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| Series: | Organics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2673-401X/6/1/7 |
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| Summary: | Nowadays, PSMA ligands are widely used for radiotheragnostic purposes in prostate cancer. The synthesis of a PSMA-Bisp conjugate was developed and realized with good yield (overall yield ~58% for the last two steps). All newly synthesized compounds were characterized by physicochemical methods: <sup>1</sup>H and <sup>13</sup>C NMR, HRMS, and LCMS (for biologically tested samples). Subsequently, Bisp1 (diacetate bispidine ligand), Bisp-alkyne (bifunctional derivative of Bisp1), and its conjugate PSMA-Bisp were labeled by <sup>64</sup>Cu in mild conditions. In vitro studies of the labeled conjugate [<sup>64</sup>Cu]Cu-PSMA-Bisp have shown great stability in model solutions. Finally, [<sup>64</sup>Cu]Cu-PSMA-Bisp was compared to the well-known PSMA-617 conjugate labeled with <sup>64</sup>Cu and they showed similar stability in excess bovine serum (BVS), and at the same time, labeling PSMA-Bisp with <sup>64</sup>Cu is characterized by extremely high kinetics in mild conditions, while labeling PSMA-617 with <sup>64</sup>Cu requires heating (90 °C). Thus, this conjugate can be incredibly promising for nuclear medicine. |
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| ISSN: | 2673-401X |