Issue 29, 2019

Modular triazine-based carborane-containing carboxylic acids – synthesis and characterisation of potential boron neutron capture therapy agents made of readily accessible building blocks

Abstract

Based on a modular combination of s-triazine, the well-known 9-mercapto-1,7-dicarba-closo-dodecaborane(12) and commercially available carboxylic acids, namely thioglycolic acid, glycine, and Nα-Boc-L-lysine, several carboxylic acid derivatives were synthesised and fully characterised. The thioglycolic acid derivative was introduced into a peptide hormone by solid phase peptide synthesis. High activity and selective internalisation into peptide receptor-expressing cells was observed. With a very high boron content of twenty boron atoms, these derivatives are interesting as selective Boron Neutron Capture Therapy (BNCT) agents.

Graphical abstract: Modular triazine-based carborane-containing carboxylic acids – synthesis and characterisation of potential boron neutron capture therapy agents made of readily accessible building blocks

Supplementary files

Article information

Article type
Paper
Submitted
20 Maijs 2019
Accepted
13 Jūn. 2019
First published
14 Jūn. 2019
This article is Open Access
Creative Commons BY-NC license

Dalton Trans., 2019,48, 10834-10844

Modular triazine-based carborane-containing carboxylic acids – synthesis and characterisation of potential boron neutron capture therapy agents made of readily accessible building blocks

M. Kellert, D. J. Worm, P. Hoppenz, M. B. Sárosi, P. Lönnecke, B. Riedl, J. Koebberling, A. G. Beck-Sickinger and E. Hey-Hawkins, Dalton Trans., 2019, 48, 10834 DOI: 10.1039/C9DT02130B

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