Synthesis and evaluation of Al18F-NODA complex conjugated 2-(4-aminophenyl)benzothiazole as a potential tumor imaging agent |
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| Affiliation: | 1. Cantab Anti-Infectives Ltd, Welwyn Garden City AL7 3AX, UK;2. Spero Therapeutics, Inc, 675 Massachusetts Avenue, 14th Floor, Cambridge, MA 02139 USA;3. Eurofins Integrated Discovery UK Ltd, Fyfield Business & Research Park, Fyfield Road, Ongar, Essex CM5 0GS, UK;1. Academician Workstation, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, Jiangxi, China;2. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China;3. College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, Jiangxi, China;1. Yncréa Hauts-de-France, Laboratory of Sustainable Chemistry and Health, Health & Environment Department, Team Sustainable Chemistry, Ecole des Hautes Etudes d’Ingénieur (HEI), UCLille, 13 rue de Toul, F-59046 Lille, France;2. Univ. Lille, Inserm, CHU Lille, Institut Pasteur de Lille, U1167 – RID-AGE – Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement, F-59000 Lille, France;3. Faculté des Sciences Pharmaceutiques et Biologiques de Lille, F-59006 Lille Cedex, France;4. Institut de Chimie des Substances Naturelles, UPR2301 CNRS, Centre de Recherche de Gif, Avenue de la Terrasse, F-91198 Gif-sur-Yvette Cedex, France;5. ‘Al. I. Cuza’ University of Iasi, Faculty of Chemistry, Bd. Carol I, nr. 11, 700506 Iasi, Romania;1. Dipartimento di Neuroscienze, Psicologia, Area del Farmaco e Salute del Bambino, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff, 6, 50019 Sesto Fiorentino, Italy;2. Scuola di Scienze del Farmaco e dei Prodotti della Salute, Università degli Studi di Camerino, Via S. Agostino 1, 62032 Camerino, MC, Italy |
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| Abstract: | ![]()
The objective of the study was to prepare and evaluate a 18F-radiolabled tracer (Al18F-5), derivated from the antitumor agent 2-(4-aminophenyl)benzothiazole, as a PET probe for tumor imaging. Al18F-5 was successfully prepared with approx. 40% radiochemical yield in aqueous phase. In in vitro cell uptake experiments and competition assay, Al18F-5 displayed good tumor-binding ability and specificity in HeLa cells (24.7 ± 0.9% ID/106 cells, IC50 = 63.8 ± 13.6 nM) and MCF-7 cells (6.8 ± 0.3% ID/106 cells, IC50 = 331.1 ± 33.7 nM). The nonradioactive compound, Al19F-5, visibly marked HeLa cells and MCF-7 cells but did not stain HEB cells in florescent staining, which further indicated the tumor-binding ability of Al18F-5. In in vivo PET imaging, HeLa and MCF-7 tumors were clearly delineated by specific accumulation of Al18F-5 in model mice. In biodistribution study, Al18F-5 exhibited good tumor uptake (4.66 ± 0.13% ID/g and 3.69 ± 0.56% ID/g, respectively), moderate tumor-to-muscle ratio (3.38 and 2.48, respectively) at 1 h post injection, which were in a good consistency with the results of PET imaging. In conclusion, Al18F-5 might be developed as a candidate PET probe for tumor imaging, though additional optimizations are still needed to improve pharmacokinetics in vivo. |
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| Keywords: | 2-(4-aminophenyl)benzothiazole PET imaging Tumor |
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