Issue 44, 2011
From the journal:

Chemical Communications

Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells†

Ellen L. Crossley,a   Fatiah Issa,a   Alana M. Scarf,b   Michael Kassiou*ab  and  Louis M. Rendina*a  

* Corresponding authors

a School of Chemistry, The University of Sydney, Sydney NSW 2006, Australia
E-mail: lou.rendina@sydney.edu.au
Fax: 61 2 9351 3329
Tel: 61 2 9351 4781

b Brain and Mind Research Institute, The University of Sydney, Camperdown, NSW 2050, Australia
E-mail: michael.kassiou@sydney.edu.au
Fax: 61 2 9351 3329
Tel: 61 2 9351 2745

Abstract

New 1,2-closo- and 7,8-nido-carboranylpyrazolopyrimidines bind to the translocator protein (TSPO) with high affinity, providing the first evidence of a unique two-site binding profile for the closo-carborane derivative. The boron-rich compounds can also deliver boron to human glioma cells far more effectively than clinical agents used in boron neutron capture therapy (BNCT).

Graphical abstract: Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells

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Article information

DOI
https://doi.org/10.1039/C1CC14587H
Article type
Communication
Submitted
27 Jul 2011
Accepted
20 Sep 2011
First published
13 Oct 2011

Chem. Commun., 2011,47, 12179-12181

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Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells

E. L. Crossley, F. Issa, A. M. Scarf, M. Kassiou and L. M. Rendina, Chem. Commun., 2011, 47, 12179 DOI: 10.1039/C1CC14587H

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