Cellular pharmacology of the D- and L-enantiomers of beta-5-o-carboranyl-2'-deoxyuridine |
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Authors: | Hurwitz S J Ma L Eleuteri A Wright J Moravek J Schinazi R F |
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Affiliation: | Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA. |
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Abstract: | The cellular pharmacology of the D- and L-enantiomers of beta-5-o-carboranyl-2'-deoxyuridine (CDU), compounds designed for boron neutron capture therapy (BNCT), were studied using human CEM lymphoblast and U-251 glioblastoma cells, at a physiologically achievable concentration (1 microM). Accumulation of the enantiomers was rapid and indistinguishable, reaching cellular concentrations > 40-fold higher than extracellular levels, with approximately 5% persisting in cells after incubation in fresh medium for more than 2 hr. Uptake was not affected by nucleoside uptake inhibitors, but was inhibited by the purine base uptake inhibitor papaverine. |
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