Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4

John J. Hall, Madhavi Sriram, Tracy E. Strecker, Justin K. Tidmore, Christopher J. Jelinek, G. D Kishore Kumar, Mallinath B. Hadimani, George Pettit, David J. Chaplin, Mary Lynn Trawick, Kevin G. Pinney

Research output: Contribution to journalArticle

22 Scopus citations

Abstract

A new trifluorinated amino-combretastatin analogue, (Z)-2-(4′-methoxy-3′-aminophenyl)-1-(3,4,5-trifluorophenyl)ethene, prepared by chemical synthesis, was found to be a potent inhibitor of tubulin assembly (IC50 = 2.9 μM), and cytotoxic against selected human cancer cell lines. This new lead compound is among the most active from a group of related structural modifications.

Original languageEnglish (US)
Pages (from-to)5146-5149
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number18
DOIs
Publication statusPublished - Sep 15 2008

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Keywords

  • Anti-cancer agents
  • Combretastatin
  • Inhibitors of tubulin assembly

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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