| Autor: |
Kellert, Martin, Friedrichs, Jan-Simon Jeshua, Ullrich, Nadine Anke, Feinhals, Alexander, Tepper, Jonas, Lönnecke, Peter, Hey-Hawkins, Evamarie |
| Jazyk: |
angličtina |
| Rok vydání: |
2021 |
| Předmět: |
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| Druh dokumentu: |
Článek |
| ISSN: |
1420-3049 |
| Popis: |
The development of novel, tumor-selective and boron-rich compounds as potential agents for use in boron neutron capture therapy (BNCT) represents a very important field in cancer treatment by radiation therapy. Here, we report the design and synthesis of two promising compounds that combine meta-carborane, a water-soluble monosaccharide and a linking unit, namely glycine or ethylenediamine, for facile coupling with various tumor-selective biomolecules bearing a free amino or carboxylic acid group. In this work, coupling experiments with two selected biomolecules, a coumarin derivative and folic acid, were included. The task of every component in this approach was carefully chosen: the carborane moiety supplies ten boron atoms, which is a tenfold increase in boron content compared to the l-boronophenylalanine (l-BPA) presently used in BNCT; the sugar moiety compensates for the hydrophobic character of the carborane; the linking unit, depending on the chosen biomolecule, acts as the connection between the tumor-selective component and the boron-rich moiety; and the respective tumor-selective biomolecule provides the necessary selectivity. This approach makes it possible to develop a modular and feasible strategy for the synthesis of readily obtainable boron-rich agents with optimized properties for potential applications in BNCT. |
| Databáze: |
Networked Digital Library of Theses & Dissertations |
| Externí odkaz: |
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