title: Cellular pharmacology of the D- and L-enantiomers of beta-5-o-carboranyl-2'-deoxyuridine.
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.
authors.affiliation: Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
authors.forename: S J
authors.initials: SJ
authors.lastname: Hurwitz
authors.forename: L
authors.initials: L
authors.lastname: Ma
authors.forename: A
authors.initials: A
authors.lastname: Eleuteri
authors.forename: J
authors.initials: J
authors.lastname: Wright
authors.forename: J
authors.initials: J
authors.lastname: Moravek
authors.forename: R F
authors.initials: RF
authors.lastname: Schinazi
mesh_terms: D001692:Biological Transport; D001896:Boron Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D002457:Cell Extracts; D002851:Chromatography, High Pressure Liquid; D003857:Deoxyuridine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D010208:Papaverine / Q000494:pharmacology; D011838:Radiation-Sensitizing Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013237:Stereoisomerism; D014407:Tumor Cells, Cultured
chemical_list: D001896:Boron Compounds; D002457:Cell Extracts; D011838:Radiation-Sensitizing Agents; C087057:5-carboranyl-2'-deoxyuridine; D010208:Papaverine; D003857:Deoxyuridine