Abstract
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.
Originalsprog | Engelsk |
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Tidsskrift | Bioorganic & Medicinal Chemistry |
Vol/bind | 13 |
Udgave nummer | 4 |
Sider (fra-til) | 1249-60 |
Antal sider | 12 |
ISSN | 0968-0896 |
DOI | |
Status | Udgivet - 15 feb. 2005 |