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).
Subject(s)
Boron Compounds/administration & dosage , Boron Neutron Capture Therapy , Drug Delivery Systems , Pyrimidines/administration & dosage , Receptors, GABA/metabolism , Antineoplastic Agents/pharmacology , Boron Compounds/chemistry , Brain Neoplasms , Cell Line, Tumor , Glioma , HEK293 Cells , Humans , Isoquinolines/pharmacology , Pyrimidines/chemistrySubject(s)
Antineoplastic Agents/metabolism , Cell Nucleus/metabolism , Coordination Complexes/metabolism , Intercalating Agents/metabolism , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Line, Tumor , Coordination Complexes/chemical synthesis , Coordination Complexes/chemistry , Fluorescent Dyes/chemistry , Gadolinium/chemistry , Humans , Intercalating Agents/chemical synthesis , Platinum/chemistry , Spectrometry, X-Ray EmissionABSTRACT
Boron Neutron Capture Therapy (BNCT) is a binary cancer treatment that exploits the short range particles released from a nuclear fission reaction involving the non-radioactive 10B nucleus and low-energy (thermal) neutrons for the destruction of tumour cells. If boronated agents are targeted towards chromosomal DNA, the efficiency of BNCT is greatly enhanced. This article presents a concise review of DNA-binding compounds that have been functionalised with boron.
Subject(s)
Boron Compounds/chemistry , Boron Neutron Capture Therapy , DNA/chemistry , Neoplasms/radiotherapy , Alkylating Agents/chemistry , Alkylating Agents/therapeutic use , Animals , Boron Compounds/therapeutic use , Humans , Intercalating Agents/chemistry , Intercalating Agents/therapeutic use , Molecular Structure , Nucleosides/chemistryABSTRACT
Reaction of the novel thiopropyl-closo-1,2-carborane ligand bearing a pendant glycerol group HS(CH(2))(3)CB(10)H(10)CCH(2)OCH(CH(2)OH)(2)(L) with the labile platinum(ii) precursor [Pt(MeCN)(terpy)](OTf)(2)(terpy = 2,2':6',2''-terpyridine; OTf = trifluoromethanesulfonate) affords the highly water-soluble platinum(ii) complex [PtL(terpy)]OTf, the first example of a metal-carborane complex functionalised with a water-solubilising glycerol group.
