Carboranyl bisglycosides for the treatment of cancer by boron neutron capture therapy

Boron neutron capture therapy is a special type of radiotherapy for the treatment of cancer by using boron compounds. Problems often arise from the: low water solubility of these compounds, their unselective uptake into the cancer cells, and their toxicity Here we describe the novel water-soluble ortho-carboranyl bisglycosides 7 and 10 containing either lactose or glucose and the mixed bisglycosides 1 and 28 containing glucose mannose, and galactose. The carboranyl bisglycosides show almost no toxicity toward bronchial carcinoma cells of line A549 up to a concentration of 0.50 mM As anticipated, these compounds exhibit nearly no uptake into C6 glioma cells; they can therefore be used for a selective delivery into malignant cells:by using conjugates of glycohydrolases and monoclonal antibodies which bind to tumor-associated antigens, since by enzymatic hydrolysis the bisglycosides are transformed into lipophilic compounds.