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Synthesis and biological evaluation of conformationally restricted and nucleobase-modified analogs of the anticancer compound 3'-C-ethynylcytidine (ECyd).

作者信息

Hrdlicka Patrick J, Jepsen Jan S, Wengel Jesper

机构信息

Nucleic Acid Center, Department of Chemistry, University of Southern Denmark, Odense M DK-5230, Denmark.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2005;24(5-7):397-400. doi: 10.1081/ncn-200059821.

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.

摘要

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