Synthesis and biological evaluation of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd) |
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Authors: | Hrdlicka Patrick J Jepsen Jan S Wengel Jesper |
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Institution: | Nucleic Acid Center, Department of Chemistry, University of Southern Denmark, Odense M DK-5230, Denmark. pjh@chem.sdu.dk |
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Abstract: | 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. |
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