Synthesis and biological evaluation of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd)
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A series of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd) and its uracil analog (EUrd) have been synthesized. While none of the conformationally restricted analogs displayed anticancer activity, 5-iodo-EUrd and 5-bromo-EUrd displayed potent anticancer activity with IC50 values of 35 nM and 0. 73 microM.
|Journal||Nucleosides, nucleotides & nucleic acids|
|Number of pages||4|
|Publication status||Published - 2005|
- Antimetabolites, Antineoplastic Agents, Cell Line, Tumor, Chemistry, Pharmaceutical, Cytidine, Drug Design, Drug Screening Assays, Antitumor, Humans, Inhibitory Concentration 50, Models, Chemical, Neoplasms, Nucleic Acid Conformation, Uracil, Uridine