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Boron Neutron Capture Therapy (BNCT) is a non-invasive binary therapeutic modality applicable to the treatment of cancers. While BNCT offers a tumor-targeting selectivity that is difficult to match by other means, the last obstacles preventing the full harness of this potential come in the form of the suboptimal boron delivery strategies presently used in the clinics. To address these challenges, we have developed delivery agents that target the glucose transporter GLUT1. Here, we present the chemical synthesis of a number of ortho-carboranylmethyl substituted glucoconjugates and the biological assessment of all positional isomers.Altogether, the study provides protocols for the synthesis and structural characterization of such glucoconjugates and insights on their essential properties e.g. cytotoxicity, GLUT1-affinity, metabolism and boron delivery capacity. In addition to solidifying the biochemical foundations of a successful GLUT1-targeting approach to BNCT, we identify the most promising modification sites in Dglucose which are critical in order to further develop this strategy towards clinical use.

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