Cytotoxic mechanisms of new antitumor nucleoside analogues, 3'-ethynylcytidine (ECyd) and 3'-ethynyluridine (EUrd)

The cytotoxic mechanisms of 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine (ECyd) and 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)uracil (EUrd) were studied with mouse mammary tumor FM3A cells and human fibrosarcoma HT1080 cells. ECyd and EUrd are converted to ECyd 5'-triphosphate (ECTP) in t...

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Bibliographic Details
Published in:	Nucleic acids symposium series (1979) no. 37; p. 137
Main Authors:	Kanda, H, Takatori, S, Matsuda, A, Sasaki, T, Tanaka, M, Fukushima, M, Wataya, Y
Format:	Journal Article
Language:	English
Published:	England 1997
Subjects:	Animals Antimetabolites, Antineoplastic - chemistry Antimetabolites, Antineoplastic - pharmacokinetics Antimetabolites, Antineoplastic - toxicity Biotransformation Cell Death - drug effects Cell Line Cytidine - analogs & derivatives Cytidine - chemistry Cytidine - pharmacokinetics Cytidine - toxicity Female Fibrosarcoma Humans Mammary Neoplasms, Experimental Mice Models, Chemical Tumor Cells, Cultured Uridine - analogs & derivatives Uridine - chemistry Uridine - pharmacokinetics Uridine - toxicity
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Summary:	The cytotoxic mechanisms of 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine (ECyd) and 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)uracil (EUrd) were studied with mouse mammary tumor FM3A cells and human fibrosarcoma HT1080 cells. ECyd and EUrd are converted to ECyd 5'-triphosphate (ECTP) in the cells. ECTP has also outstanding stability in the cells; the half life of ECTP in FM3A cells was more than 3 days. The metabolisms and mechanisms of these analogues may play a key role in a potent antitumor activities against slow-growing solid tumors.
ISSN:	0261-3166