Abstract:
:Fluorinated nucleoside analogues are a major class of cancer chemotherapy agents, and include the drugs 5-fluorouracil (5FU) and 5-fluoro-2'-deoxyuridine (FdUrd). The aim of this study was to examine the cellular toxicity of two novel fluorinated pyrimidine L-nucleosides that are enantiomers of D-nucleosides and may be able to increase selectivity for cancer cells as a result of their unnatural L-configuration. Two fluorinated pyrimidine L-nucleosides were examined in this study, L110 ([β-L, β-D]-5-fluoro-2'-deoxyuridine) and L117 (β-L-deoxyuridine:β-D-5'-fluoro-2'-deoxyuridine). The cytotoxicity of these L-nucleoside was determined in primary mouse fibroblasts and was compared with 5FU and FdUrd. In addition, the influence of p53 status on cytotoxicity was investigated. These cytotoxicity assays were performed on a matched set of primary mouse fibroblasts that were either wild type or null for the p53 tumour suppressor gene. It was found that cells lacking functional p53 were over 7500 times more sensitive to the drugs L110, L117 and FdUrd than cells containing wild type p53.
journal_name
Chem Biol Interactjournal_title
Chemico-biological interactionsauthors
Murray V,Taylor CB,Gero AM,Lutze-Mann LHdoi
10.1016/j.cbi.2015.08.010subject
Has Abstractpub_date
2015-10-05 00:00:00pages
102-9eissn
0009-2797issn
1872-7786pii
S0009-2797(15)30038-7journal_volume
240pub_type
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