Cellular pharmacology of the D- and L-enantiomers of beta-5-o-carboranyl-2'-deoxyuridine.
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.
Hurwitz
S J
SJ
Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Ma
L
L
Eleuteri
A
A
Wright
J
J
Moravek
J
J
Schinazi
R F
RF
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
D001896:Boron Compounds; D002457:Cell Extracts; D011838:Radiation-Sensitizing Agents; C087057:5-carboranyl-2'-deoxyuridine; D010208:Papaverine; D003857:Deoxyuridine