Synthesis and evaluation of 18F-labeled tertiary benzenesulfonamides for imaging carbonic anhydrase IX expression in tumours with positron emission tomography |
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| Affiliation: | 1. Department of Neuroradiology, Eberhard Karls University Tübingen, Hoppe-Seyler-Str. 3, Tübingen 72076, Germany;2. Department of Diagnostic and Interventional Radiology, Eberhard Karls University Tübingen, Tübingen, Germany;3. Department of Internal Medicine—Oncology, Eberhard Karls University Tübingen, Tübingen, Germany;1. Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Groningen, the Netherlands;2. Stratingh Institute for Chemistry, University of Groningen, Groningen, the Netherlands |
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| Abstract: | Three tertiary benzenesulfonamide inhibitors 4a–c were radiolabeled with 18F and evaluated for imaging carbonic anhydrase IX (CA IX) expression with positron emission tomography. All three inhibitors exhibit <10 nM affinity for CA IX with no measurable affinity for CA II. Despite good affinity/selectivity to CA IX and excellent stability in plasma, uptake of [18F]4a–c in CA IX-expressing HT-29 tumours was low without significant contrast. [18F]4a,b were excreted rapidly, while [18F]4c exhibited significant in vivo defluorination leading to high bone uptake. Due to minimal uptake in HT-29 tumours compared to normal organs/tissues, 18F-labeled benzenesulfonamides [18F]4a–c are not suitable as CA IX imaging agents. |
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| Keywords: | Carbonic anhydrase IX Tertiary benzenesulfonamides Fluorine-18 In vivo defluorination Positron emission tomography |
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