Sweet Battle of the EpimersâContinued Exploration of Monosaccharide-Derived Delivery Agents for Boron Neutron Capture Therapy.
Mol Pharm
; 20(6): 3127-3139, 2023 06 05.
Article
em En
| MEDLINE
| ID: mdl-37134022
ABSTRACT
Boron neutron capture therapy (BNCT) is a cancer therapy in which boron delivery agents play a crucial role. In theory, delivery agents with high tumor targeting capabilities can lead to selective eradication of tumor cells without causing harmful side effects. We have been working on a GLUT1-targeting strategy to BNCT for a number of years and found multiple promising hit compounds which outperform the clinically employed boron delivery agents in vitro. Herein, we continue our work in the field by further diversification of the carbohydrate scaffold in order to map the optimal stereochemistry of the carbohydrate core. In the sweet battle of the epimers, carborane-bearing d-galactose, d-mannose, and d-allose are synthesized and subjected to in vitro profiling studiesâwith earlier work on d-glucose serving as the reference. We find that all of the monosaccharide delivery agents display a significantly improved boron delivery capacity over the delivery agents approved for clinical use in vitro, thus providing a sound foundation for advancing toward in vivo preclinical assessment studies.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Boranos
/
Terapia por Captura de Nêutron de Boro
/
Neoplasias
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article