ABSTRACT
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
A series of novel, dinuclear (2,2':6',2''-terpyridine)platinum(ii) complexes containing bis(thioalkyl)-dicarba-closo-dodecaborane(12)(carborane) ligands were prepared and characterised, and their preliminary anti-cancer characteristics have been determined in vitro; the complexes are the first examples of bis-intercalator complexes containing a boron-rich carborane cage.
Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Boranes/chemistry , Boranes/pharmacology , Platinum Compounds/chemistry , Platinum Compounds/pharmacology , Animals , Antineoplastic Agents/chemical synthesis , Boranes/chemical synthesis , Cell Line, Tumor , Drug Resistance, Neoplasm , Inhibitory Concentration 50 , Leukemia/drug therapy , Ligands , Molecular Structure , Platinum Compounds/chemical synthesis , Structure-Activity RelationshipABSTRACT
A series of novel platinum(II)-2,2':6',2' '-terpyridine (trpy) complexes containing (thioalkyl)dicarba-closo-dodecaborane(12) (closo-carborane) derivatives were prepared by treatment of the labile precursor species [Pt(MeCN)(trpy)](OTf)2 with R(CH2)nSH (R = closo-1,2-carborane, n = 0-3; R = closo-1,7-carborane, n = 1; R = closo-1,12-carborane, n = 1) in the presence of NEt3 to afford brightly colored complexes of the type [PtS(CH2)nR(trpy)]OTf. All products were characterized by means of multinuclear (1H, 13C, 11B, and 195Pt) 1D- and 2D-NMR spectroscopy, ESI-MS, and, for the 1,7-carborane derivative, X-ray crystallography. Preliminary in vitro cytotoxicity studies of selected complexes against human ovarian carcinoma cells are also reported.
