Antitumor mechanisms and metabolism of the novel antitumor nucleoside analogues, 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine and 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)uracil

@article{Takatori1999AntitumorMA,
  title={Antitumor mechanisms and metabolism of the novel antitumor nucleoside analogues, 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine and 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)uracil},
  author={Satoshi Takatori and Hiroshi Kanda and Kiyoko Takenaka and Yusuke Wataya and Akira Matsuda and Masakazu Fukushima and Yuji Shimamoto and Motohiro Tanaka and Takuma Sasaki},
  journal={Cancer Chemotherapy and Pharmacology},
  year={1999},
  volume={44},
  pages={97-104}
}
The antitumor ribonucleoside analogues 1-(3-C-ethynyl-β-d-ribo-pentofuranosyl)cytosine (ECyd) and 1-(3-C-ethynyl-β-d-ribo-pentofuranosyl)uracil (EUrd), first synthesized in 1995, have strong antitumor activity against human cancer xenografts without severe side effects. Here, we studied the antitumor mechanisms of ECyd and EUrd using mouse mammary tumor FM3A cells in vitro and the mechanism of selective cytotoxicity of ECyd using human tumor xenografts in nude rats in vivo. In FM3A cells, ECyd… CONTINUE READING

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EUrd and its derivatives were minor metabolites in the cells treated with ECyd , so cytidine forms probably were not converted to uridine forms at the nucleoside or nucleotide stage .
EUrd and its derivatives were minor metabolites in the cells treated with ECyd , so cytidine forms probably were not converted to uridine forms at the nucleoside or nucleotide stage .
EUrd and its derivatives were minor metabolites in the cells treated with ECyd , so cytidine forms probably were not converted to uridine forms at the nucleoside or nucleotide stage .
ECyd - phosphorylating activity ( uridine / cytidine kinase ) in the xenografts was higher than that in the organs of the rats .
CytosineNo subtypeUracil
Probably the uracil moieties of EUrd derivatives were efficiently converted to cytosine moieties in the cells .
UracilNo subtypeCytosine
Probably the uracil moieties of EUrd derivatives were efficiently converted to cytosine moieties in the cells .
EUrd and its derivatives were minor metabolites in the cells treated with ECyd , so cytidine forms probably were not converted to uridine forms at the nucleoside or nucleotide stage .
EUrd and its derivatives were minor metabolites in the cells treated with ECyd , so cytidine forms probably were not converted to uridine forms at the nucleoside or nucleotide stage .
EUrd and its derivatives were minor metabolites in the cells treated with ECyd , so cytidine forms probably were not converted to uridine forms at the nucleoside or nucleotide stage .
EUrd and its derivatives were minor metabolites in the cells treated with ECyd , so cytidine forms probably were not converted to uridine forms at the nucleoside or nucleotide stage .
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