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.

Per Anhalter in den Zellkern: Ein in DNA intercalierter Metallkomplex kann die selektive Ansammlung eines intakten Wirkstoffs in den Kernen von humanen Lungenkrebszellen (A549) ermöglichen. Mit einem Platinkomplex gelang es nun, auf diesem Weg Gadolinium in Zellkerne zu schleusen. Die Synchrotron‐Röntgenfluoreszenz‐Bildgebung diente zum Nachweis des Prozesses (siehe Bilder).

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.

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).

Hitching a ride: Treatment of A549 human lung carcinoma cells with a DNA metallointercalator complex results in the selective aggregation of the intact drug within the cell nuclei, as determined by synchrotron X‐ray fluorescence (XRF) imaging (see images). This work is the first example of gadolinium delivery by a platinum complex to a tumor‐cell nucleus.