Abstract
Boron neutron capture therapy (BNCT) is a binary type of radiotherapy for the treatment of cancer. Due to recent developments of neutron accelerators and their installation in some hospitals, BNCT is on the rise worldwide and is expected to have a significant impact on patient treatments. Therefore, there is an increasing need for improved boron delivery agents. Among the many small molecules and delivery systems developed, a significant amount of recent research focused on the synthesis of boron-containing sugar and amino acid derivatives to exploit specific transport proteins, as d-glucose transporter 1 (GLUT1) and large neutral amino acid transporter (LAT1), overexpressed by tumor cells. This review will discuss the last year’s achievements in the synthesis and some biological evaluation of boronated sugars derivatives. The compounds described in this review are intrinsically asymmetric due to the presence of chiral sugar moieties, often joined to boron clusters, which are structural elements with high symmetry.
Highlights
Boron neutron capture therapy (BCNT) is a binary radiotherapeutic approach based on the nuclear capture of low-energy neutrons by a boron-10 (10 B) nucleus. 10 B has a cross-section for neutron capture of 3840 barns (1 barn = 10−24 m2, the size of the uranium nucleus Mughabghab, S.F. (2003), ‘Thermal neutron capture cross-sections: Resonance integrals and g- factors’, IAEA Nuclear Data Section, Wagramer Strasse 5, A-1400, Vienna), by far greater than that of the elements commonly present in tissues.When B captures a neutron, the formed B isotope is in an excited state which rapidly decays through a fission reaction producing an α particle and recoiling a lithium7 (7 Li) ion
The results strongly suggest that absorption of these products is achieved through glucose transporter 1 (GLUT1)
As with many other conventional antitumor drugs, and for Boron neutron capture therapy (BNCT), predictably there will not be a universal boron carrier, but more compounds will probably be needed for the treatment of different tumors
Summary
If a 10 B-containing compound is preferentially accumulated within a cancer cell, the irradiation of the tumor area with a neutron flux gives rise to a lethal fission reaction confined within the boron-containing cells, providing selective destruction of the malignant cells saving the surrounding healthy tissues, provided that some requirements are fulfilled, as later discussed (Figure 1). At the same time Soloway, again at the Massachusetts General Hospital, began studies for finding suitable non-toxic boron-containing compounds These experiments failed essentially for a lack of selectivity of boron compounds used, together with the low penetration of thermal neutrons. For these reasons, the use of epithermal neutrons that are thermalized by water in the patient’s tissues when they arrive proximal to the tumor site was introduced. Boron clusters have attracted great interest, forcing chemists to
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