Synthesis and in vitro evaluation of a novel radioligand for αvβ3 integrin receptor imaging: [¹⁸F]FPPA-c(RGDfK)
- Monaco, Alessandra Cyclotron Unit, University Hospital of Geneva, Switzerland - School of Pharmaceutical Sciences, University of Geneva and University of Lausanne, Switzerland
- Zoete, Vincent Swiss Institute of Bioinformatics, University of Lausanne, Switzerland
- Alghisi, Gian Carlo University of Lausanne, Division of Experimental Oncology, Multidisciplinary Oncology Center, Switzerland
- Rüegg, Curzio University of Lausanne, Division of Experimental Oncology, Multidisciplinary Oncology Center, Switzerland - University of Fribourg, Faculty of Science, Department of Medicine, Switzerland
- Michelin, Olivier Swiss Institute of Bioinformatics, University of Lausanne, Switzerland
- Prior, John CHUV, Department of Nuclear Medicine, Lausanne, Switzerland
- Scapozza, Leonardo School of Pharmaceutical Sciences, University of Geneva and University of Lausanne, Switzerland
- Seimbille, Yann Cyclotron Unit, University Hospital of Geneva, Switzerland - School of Pharmaceutical Sciences, University of Geneva and University of Lausanne, Switzerland
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15.11.2013
Published in:
- Bioorganic & Medicinal Chemistry Letters. - 2013, vol. 23, no. 22, p. 6068–6072
English
The development of RGD-based antagonist of αvβ3 integrin receptor has enhanced the interest in PET probes to image this receptor for the early detection of cancer, to monitor the disease progression and the response to therapy. In this work, a novel prosthetic group (N-(4-fluorophenyl)pent-4-ynamide or FPPA) for the 18F-labeling of an αvβ3 selective RGD-peptide was successfully prepared. [18F]FPPA was obtained in three steps with a radiochemical yield of 44% (decay corrected). Conjugation to c(RGDfK(N3)) by the Cu(II) catalyzed Huisgen azido alkyne cycloaddition provided the [18F]FPPA-c(RGDfK) with a radiochemical yield of 29% (decay corrected), in an overall synthesis time of 140 min.
- Faculty
- Faculté des sciences et de médecine
- Department
- Médecine 3ème année
- Language
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- English
- Classification
- Biological sciences
- License
- License undefined
- Identifiers
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- RERO DOC 209503
- DOI 10.1016/j.bmcl.2013.09.031
- Persistent URL
- https://folia.unifr.ch/unifr/documents/303401
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