Towards carborane-functionalised structures for the treatment of brain cancer

Authors:   Gianpiero Calabrese, Anis Daou, Eugen Barbu, John Tsibouklis
Journal: Drug Discovery Today
https://doi.org/10.1016/j.drudis.2017.08.009
Abstract: Boron neutron capture therapy (BNCT) is a promising targeted chemoradiotherapeutic technique for the management of invasive brain tumors, such as glioblastoma multiforme (GBM). A prerequisite for effective BNCT is the selective targeting of tumour cells with 10B-rich therapeutic moieties. To this end, polyhedral boranes, especially carboranes, have received considerable attention because they combine a high boron content with relative low toxicity and metabolic inertness. Here, we review progress in the molecular design of recently investigated carborane derivatives in light of the widely accepted performance requirements for effective BNCT.