期刊
DALTON TRANSACTIONS
卷 49, 期 1, 页码 57-69出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9dt04031e
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资金
- Europaischer Fonds for regionale Entwicklung (EFRE)
- European Union
- Free State of Saxony (ESF)
- [SFB 1052]
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 bio-molecules 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-Phe(6), beta-Ala(11), Ala(13), Nle(14)]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.
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