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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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  • Patrick J Hrdlicka
  • Jan S Jepsen
  • Claus Nielsen
  • Jesper Wengel
  • Stenvang, Jan
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.
OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry
Vol/bind13
Udgave nummer4
Sider (fra-til)1249-60
Antal sider12
ISSN0968-0896
DOI
StatusUdgivet - 15 feb. 2005

ID: 59323719