Organotrifluoroborate Sugar Conjugates for a Guided Boron Neutron Capture Therapy


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.


Laura Confalonieri, Daniela Imperio, Alvaro Erhard, Silvia Fallarini, Federica Compostella,
Erika del Grosso, Marcin Balcerzyk and Luigi Panza

Published: 12 Dec 2022


To cite this article:
ACS Omega 2022, 7, 51, 48340–48348
Publication Date:December 12, 2022
Copyright © 2022 The Authors. Published by American Chemical Society

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