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Issue 1, 2020

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

Supplementary files

Article information


Submitted
14 Oct 2019
Accepted
26 Nov 2019
First published
26 Nov 2019

This article is Open Access

Dalton Trans., 2020,49, 57-69
Article type
Paper

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, 49, 57 DOI: 10.1039/C9DT04031E

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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