Abstract
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.
| Original language | English |
|---|---|
| Pages (from-to) | 6068-6072 |
| Number of pages | 5 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 23 |
| Issue number | 22 |
| DOIs | |
| Publication status | Published - 15 Nov 2013 |
| Externally published | Yes |
Bibliographical note
Funding Information:This research was carried out at the cyclotron unit of the University Hospital of Geneva , using resources were provided by the Center of Biomedical Imaging (CIBM) , the MS facility of the University of Geneva . This work was supported by the Leenaards Foundation . We would like to thank Dr. Sébastien Tardy for helpful discussion and Dr. Elisabeth Rivara-Minten, for her support at the NMR facility.
