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
  • 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.