Carboranyl Bisglycosides for the Treatment of Cancer by Boron Neutron Capture Therapy

摘要

Boron neutron capture therapy is a special type of radiotherapy for the treatment of cancer by using boron compounds. Problems often arise from the 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 latose or glucose and the mixed bisglycosides 1 and 28 containing glucose, mannose, and galactose. The carboranyl bisglycosdies show almsot no toxicity toward bronchial carbinoma cells of line A549 up to a concentration of 0.50 mM. As anticipated, these compounds exhibit nearly no uptkae 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 tumorassociated antigens, since by enzymatic hydrolysis the bisglycosides are transformed into lipophilic compounds.