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Tuning a modular system – synthesis and characterisation of a boron-rich s-triazine-based carboxylic acid and amine bearing a galactopyranosyl moiety

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Abstract

Introduction of a bis(isopropylidene)-protected galactopyranosyl moiety in s-triazine-based boron-rich carboxylic acids and amines results in soluble and suitable coupling partners for tumour-selective biomolecules with applications as selective agents for boron neutron capture therapy (BNCT). Bearing either a carboxylic acid or primary amine as a functional group, these compounds are highly versatile and thus largely extend the possible coupling strategies with suitable biomolecules. Modification of the gastrin-releasing peptide receptor (GRPR) selective agonist [D-Phe6, β-Ala11, Ala13, Nle14]Bn(6–14) with the carboxylic acid derivative yielded a bioconjugate with an optimal receptor activation and internalisation profile. This demonstrates the great potential of this approach for the development of novel boron delivery agents.

Graphical abstract: Tuning a modular system – synthesis and characterisation of a boron-rich s-triazine-based carboxylic acid and amine bearing a galactopyranosyl moiety

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Publication details

The article was received on 14 Oct 2019, accepted on 26 Nov 2019 and first published on 26 Nov 2019


Article type: Paper
DOI: 10.1039/C9DT04031E
Dalton Trans., 2020, Advance Article
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    Tuning a modular system – synthesis and characterisation of a boron-rich s-triazine-based carboxylic acid and amine bearing a galactopyranosyl moiety

    M. Kellert, P. Hoppenz, P. Lönnecke, D. J. Worm, B. Riedl, J. Koebberling, A. G. Beck-Sickinger and E. Hey-Hawkins, Dalton Trans., 2020, Advance Article , DOI: 10.1039/C9DT04031E

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