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; Fatiah Issa; Alana M Scarf; Michael Kassiou; Louis M Rendina

doi:10.1039/c1cc14587h

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

Chem Commun (Camb). 2011 Nov 28;47(44):12179-81. doi: 10.1039/c1cc14587h. Epub 2011 Oct 13.

Authors

Ellen L Crossley¹, Fatiah Issa, Alana M Scarf, Michael Kassiou, Louis M Rendina

Affiliation

¹ School of Chemistry, The University of Sydney, Sydney NSW 2006, Australia.

PMID: 21993200
DOI: 10.1039/c1cc14587h

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).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / pharmacology
Boron Compounds / administration & dosage*
Boron Compounds / chemistry
Boron Neutron Capture Therapy*
Brain Neoplasms
Cell Line, Tumor
Drug Delivery Systems*
Glioma
HEK293 Cells
Humans
Isoquinolines / pharmacology
Pyrimidines / administration & dosage*
Pyrimidines / chemistry
Receptors, GABA / metabolism*

Substances

Antineoplastic Agents
Boron Compounds
Isoquinolines
Pyrimidines
Receptors, GABA
TSPO protein, human
PK 11195