1. Supplementary Information 'Organotrifluoroborate Sugar Conjugates for a Guided Boron Neutron Capture Therapy: from Synthesis to Positron Emission Tomography'
- Author
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Imperio, Daniela [daniela.imperio@uniupo.it], Balcerzyk, Marcin [mbalcerzyk@us.es], Confalonieri, Laura, Imperio, Daniela, Erhard, Álvaro, Fallarini, Silvia, Compostella, Federica, Del Grosso, Erika, Balcerzyk, Marcin, Panza, Luigi, Imperio, Daniela [daniela.imperio@uniupo.it], Balcerzyk, Marcin [mbalcerzyk@us.es], Confalonieri, Laura, Imperio, Daniela, Erhard, Álvaro, Fallarini, Silvia, Compostella, Federica, Del Grosso, Erika, Balcerzyk, Marcin, and Panza, Luigi
- Abstract
Sugars are a versatile tool for targeting malignant cells and have been extensively used for drug delivery and imaging techniques. Their prototype, fluorodeoxyglucose ([18F]FDG), is currently used for positron emission tomography. Boron neutron capture therapy (BNCT) is a cancer treatment that relies on irradiation with thermal neutrons of cancer cells previously loaded with [10B]-containing compounds. The recent introduction of accelerators as a neutron source for clinical use prompts the planning of delivery compounds enriched with boron able to be traced in real time. This work describes the first synthesis of a new class of sugar derivatives conjugated to a trifluoroborate moiety as potential theranostic agents. Stability and cytotoxicity studies are reported for all compounds, together with [18F] radiolabeling optimization and in vivo preliminary positron emission tomography (PET) experiments on a selected compound.
- Published
- 2022