closo-ortho-carborane-based glucosamine derivative

The closo-ortho-carborane-based glucosamine derivative, also known as compound 4, is an experimental small-molecule boron delivery agent designed for Boron Neutron Capture Therapy (BNCT). It consists of a glucosamine (N-acetylglucosamine) scaffold conjugated to a closo-ortho-carborane boron cluster via click chemistry. The compound is designed to target the glucose transporters GLUT-1 and GLUT-2, which are overexpressed in various tumor cells, to facilitate selective boron accumulation in malignant tissues. Preclinical studies in glioblastoma (U87-MG) and melanoma (A375) cell lines have shown that the compound effectively enriches cells with boron without significant toxicity at concentrations up to 100 µM. Its water solubility (4.669 g/L) supports intravenous administration, positioning it as a potential alternative to the current BNCT standard, boronophenylalanine (BPA). The compound was developed by researchers at the University of Eastern Piedmont and the National Institute of Nuclear Physics (INFN) and was first described in the journal Pharmaceuticals in June 2025.

Other names

compound 4compound4compound-4GlcNAc-carborane conjugate