Organotrifluoroborate Sugar Conjugates for a Guided Boron Neutron Capture Therapy: From Synthesis to Positron Emission Tomography.
Laura ConfalonieriDaniela ImperioAlvaro ErhardSilvia FallariniFederica CompostellaErika Del GrossoMarcin BalcerzykLuigi PanzaPublished in: ACS omega (2022)
Sugars are a versatile tool for targeting malignant cells and have been extensively used for drug delivery and imaging techniques. Their prototype, fluorodeoxyglucose ([ 18 F]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 [ 10 B]-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 [ 18 F] radiolabeling optimization and in vivo preliminary positron emission tomography (PET) experiments on a selected compound.
Keyphrases
- positron emission tomography
- computed tomography
- drug delivery
- cancer therapy
- pet ct
- pet imaging
- photodynamic therapy
- induced apoptosis
- high resolution
- cell cycle arrest
- multidrug resistant
- fluorescence imaging
- radiation therapy
- stem cells
- cell proliferation
- oxidative stress
- risk assessment
- bone marrow
- cell therapy
- drug release
- wound healing
- case control
- pi k akt
- monte carlo
- iron oxide