Development of PSMA-1007-related series of 18F-labeled Glu-Ureido-type PSMA inhibitors
In recent years, a number of drugs targeting the prostate-specific membrane antigen (PSMA) have become important tools in the diagnosis and treatment of prostate cancer. In the present work, we report on the synthesis and preclinical evaluation of a series of 18F-labeled PSMA ligands for diagnostic...
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| Hauptverfasser: | , , , , , , , , , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
August 27, 2020
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| In: |
Journal of medicinal chemistry
Year: 2020, Jahrgang: 63, Heft: 19, Pages: 10897-10907 |
| ISSN: | 1520-4804 |
| DOI: | 10.1021/acs.jmedchem.9b01479 |
| Online-Zugang: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1021/acs.jmedchem.9b01479
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| Verfasserangaben: | Jens Cardinale, Mareike Roscher, Martin Schäfer, Max Geerlings, Martina Benešová, Ulrike Bauder-Wüst, Yvonne Remde, Matthias Eder, Zora Nováková, Lucia Motlová, Cyril Barinka, Frederik L. Giesel, and Klaus Kopka |
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| 520 | |a In recent years, a number of drugs targeting the prostate-specific membrane antigen (PSMA) have become important tools in the diagnosis and treatment of prostate cancer. In the present work, we report on the synthesis and preclinical evaluation of a series of 18F-labeled PSMA ligands for diagnostic application based on the theragnostic ligand PSMA-617. By applying modifications to the linker structure, insight into the structure-activity relationship could be gained, highlighting the importance of hydrophilicity and stereoselectivity on interaction with PSMA and hence the biodistribution. Selected compounds were co-crystallized with the PSMA protein and analyzed by X-rays with mixed results. Among these, PSMA-1007 (compound 5) showed the best interaction with the PSMA protein. The respective radiotracer [18F]PSMA-1007 was translated into the clinic and is, in the meantime, subject of advanced clinical trials. | ||
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