2. Academic Validation
  3. Synthesis of novel 7-oxo and 7-hydroxy trifluoroallocolchicinoids with cytotoxic effect

Synthesis of novel 7-oxo and 7-hydroxy trifluoroallocolchicinoids with cytotoxic effect

  • Bioorg Med Chem. 2012 Apr 15;20(8):2614-23. doi: 10.1016/j.bmc.2012.02.043.
Elizabeth Chosson 1,  Francesca Santoro,  Christophe Rochais,  Jana Sopkova-de Oliveira Santos,  Rémi Legay,  Sylviane Thoret,  Thierry Cresteil,  Maria Stefania Sinicropi,  Thierry Besson,  Patrick Dallemagne
Affiliations

Affiliation

  • 1 Université de Caen Basse Normandie, Centre d'Etudes et de Recherche sur le Médicament de Normandie UPRES EA 4258 - FR CNRS 3038 INC3M, UFR des Sciences Pharmaceutiques, Bd Becquerel, 14032 Caen cedex, France.
PMID: 22429510 DOI: 10.1016/j.bmc.2012.02.043
Abstract

The synthesis of 7-oxo and 7-hydroxy trifluoroallocolchicinoids was achieved through the intramolecular cyclization of o-phenyl-β-phenylalanines. The resulting compounds were evaluated for their cytotoxic activity against KB cells and their inhibitory effect towards the polymerization of tubulin. The results yielded some potent cytotoxic compounds with correlated partial antitubulin effect.

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