Synthesis and biological evaluation of nucleobase-modified analogs of the anticancer compounds 3'-C-ethynyluridine (EUrd) and 3'-C-ethynylcytidine (ECyd)
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A series of nucleobase-modified analogs of the anticancer compounds 3'-C-ethynyluridine (EUrd) and 3'-C-ethynylcytidine (ECyd) were designed to overcome the strict substrate specificity of the activating uridine-cytidine kinase. EUrd, ECyd and target nucleosides were obtained using a short convergent synthetic route utilizing diacetone-alpha-D-glucose as starting material. 5-Iodo-substituted EUrd was the most potent inhibitor among the novel nucleobase-modified analogs in in vitro assays against human adenocarcinoma breast and prostate cancer cells with IC50 values down to 35 nM.
Original language | English |
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Journal | Bioorganic & Medicinal Chemistry |
Volume | 13 |
Issue number | 4 |
Pages (from-to) | 1249-60 |
Number of pages | 12 |
ISSN | 0968-0896 |
DOIs | |
Publication status | Published - 15 Feb 2005 |
- Antineoplastic Agents, Cell Line, Tumor, Cytidine, Drug Screening Assays, Antitumor, Humans, Magnetic Resonance Spectroscopy, Uridine
Research areas
ID: 59323719