title: Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells.
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).
authors: School of Chemistry, The University of Sydney, Sydney NSW 2006, Australia.
authors: Ellen L
authors: EL
authors: Crossley
authors: Fatiah
authors: F
authors: Issa
authors: Alana M
authors: AM
authors: Scarf
authors: Michael
authors: M
authors: Kassiou
authors: Louis M
authors: LM
authors: Rendina
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D001896:Boron Compounds / Q000008:administration & dosage* / Q000737:chemistry; D016754:Boron Neutron Capture Therapy; D001932:Brain Neoplasms; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D005910:Glioma; D057809:HEK293 Cells; D006801:Humans; D007546:Isoquinolines / Q000494:pharmacology; D011743:Pyrimidines / Q000008:administration & dosage* / Q000737:chemistry; D018079:Receptors, GABA / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D001896:Boron Compounds; D007546:Isoquinolines; D011743:Pyrimidines; D018079:Receptors, GABA; C499229:TSPO protein, human; C037850:PK 11195