2. Academic Validation
  3. C5-Modified nucleosides exhibiting anticancer activity

C5-Modified nucleosides exhibiting anticancer activity

  • Bioorg Med Chem Lett. 2009 Aug 15;19(16):4688-91. doi: 10.1016/j.bmcl.2009.06.072.
Yoon-Suk Lee 1,  Sun Min Park,  Hwan Mook Kim,  Song-Kyu Park,  Kiho Lee,  Chang Woo Lee,  Byeang Hyean Kim
Affiliations

Affiliation

  • 1 Department of Chemistry, BK School of Molecular Science, Pohang University of Science and Technology, Pohang 790-784, Republic of Korea.
PMID: 19596579 DOI: 10.1016/j.bmcl.2009.06.072
Abstract

We describe (i) a simple method for the synthesis of C5-modified nucleosides from 5-iodo-2'-deoxyuridine and (ii) their activity against six types of human Cancer cell lines (HCT15, MM231, NCI-H23, NUGC-3, PC-3, ACHN). We generated nitrile oxides in situ from oximes using a commercial bleaching agent; their cycloadditions with 5-ethynyl-2'-deoxyuridine yielded isoxazole derivatives possessing activity against the Cancer cell lines. We synthesized several azides from benzylic bromides and their click reactions with 5-ethynyl-2'-deoxyuridine provided triazole derivatives.

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