2. Academic Validation
  3. Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4

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

  • Bioorg Med Chem Lett. 2008 Sep 15;18(18):5146-9. doi: 10.1016/j.bmcl.2008.07.070.
John J Hall 1,  Madhavi Sriram,  Tracy E Strecker,  Justin K Tidmore,  Christopher J Jelinek,  G D Kishore Kumar,  Mallinath B Hadimani,  George R Pettit,  David J Chaplin,  Mary Lynn Trawick,  Kevin G Pinney
Affiliations

Affiliation

  • 1 Department of Chemistry and Biochemistry, Baylor University, One Bear Place #97348, Waco, TX 76798-7348, USA.
PMID: 18710804 DOI: 10.1016/j.bmcl.2008.07.070
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 (IC(50)=2.9 microM), and cytotoxic against selected human Cancer cell lines. This new lead compound is among the most active from a group of related structural modifications.

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