Speaker
Description
Molecular imaging holds the promise of non-invasive assessment for biological and biochemical processes in living subjects using specific imaging tracers. Positron Emission Tomography (PET) is a highly specific and sensitive molecular imaging technique with widespread use for research and clinical application. The majority of PET studies today are performed with molecules labelled with fluorine-18, a radionuclide possessing important characteristics including a favourable half-life (110 min) and the ability to replace H in organic molecules.1
It’s widely recognised that porphyrins are one of the most important prosthetic groups in biological systems and porphyrin derivatives have recently found promising biomedical applications in detection and treatment of a variety of tumours due to their affinities for these tissues in relation with the nature of the side chain and the mechanism of their physico-chemical action.2-5 In this communication we describe our recent studies on the synthesis of novel sulfonamide substituted meso-tetraphenylporphyrins and automated synthesis of new 18F-labelled porphyrin derivatives, by fluorination via nucleophilic substitution with K2CO3/K2.2.2/ACN. Preliminary biodistribution studies in rats with PET will be presented. We believe our results may open new directions for the development of new theragnostic tools.
Acknowlegments:
The authors thank FCT/QREN/FEDER-COMPETE Portugal; FCT for AVC Simoes PhD grant (SFRH/BD/65699/2009); Maria Puigivila, Carlos Perez, Mikel González and Aitor Lekuona from CICbiomaGUNE.
References
1 William K. Hagmann, Journal of Medicinal Chemistry, 15, 2008, 4359; (b) Didier Le Bars, Journal of Fluorine Chemistry, 127, 2006, 1488.
[2] Dabrowski et al., ChemMedChem, 2011, 6, 1715
[3] M. M. M Pereira, C. J. P Monteiro, A. V. C. Simões; et al., J. Porphyrins Phathlocyanines 13, 2009, 567.
[4] Dabrowski et al., Med. Chem. Commun., 3, 2012, 502.
[5] Pereira, M. M.; Monteiro, C. J. P.; Simoes, A. V. C.; et al., Tetrahedron, 66, 2010, 9545.
