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Bioorg Med Chem Lett. 2014 Apr 1;24(7):1758-61. doi: 10.1016/j.bmcl.2014.02.035. Epub 2014 Feb 24.

Design, synthesis and biological evaluation of new inhibitors of Bax/Bcl-xL interaction in cancer cells.

Author information

  • 1Université de Rennes 1, Institut des Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France.
  • 2UMR 892 INSERM/6299 CNRS/Université de Nantes, Team 8 "Cell survival and tumor escape in breast cancer", Institut de Recherche Thérapeutique de l'Université de Nantes, 8 quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France; Institut de Cancérologie de l'Ouest, Centre de Lutte contre le Cancer René Gauducheau, Boulevard Jacques Monod, 44805 Saint Herblain-Nantes Cedex, France; Plateforme IMPACT®, Biogenouest Institut de Recherche Thérapeutique de l'Université de Nantes, 8 quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France.
  • 3UMR 892 INSERM/6299 CNRS/Université de Nantes, Team 8 "Cell survival and tumor escape in breast cancer", Institut de Recherche Thérapeutique de l'Université de Nantes, 8 quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France.
  • 4UMR 892 INSERM/6299 CNRS/Université de Nantes, Team 8 "Cell survival and tumor escape in breast cancer", Institut de Recherche Thérapeutique de l'Université de Nantes, 8 quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France; Institut de Cancérologie de l'Ouest, Centre de Lutte contre le Cancer René Gauducheau, Boulevard Jacques Monod, 44805 Saint Herblain-Nantes Cedex, France.
  • 5Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint Grégoire, France.
  • 6Université de Rennes 1, Institut des Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France. Electronic address: Rene.Gree@univ-rennes1.fr.

Abstract

We describe the synthesis of a series of new molecules containing phenol and triazoles moieties, compounds which have been evaluated for their ability to inhibit Bax/Bcl-xL interactions in cancer cells, by using BRET assays, and to induce cell death. Several derivatives exhibit a very promising activity, being more potent than the reference compounds acylpyrogallol A and ABT-737. These preliminary results demonstrate that derivatives of this family can be attractive to develop new molecules with potent anticancer activity.

Copyright © 2014 Elsevier Ltd. All rights reserved.

KEYWORDS:

Apoptosis; BRET; Bax; Bcl-xL; Cancer; Polyphenol; Triazoles

PMID:
24602902
[PubMed - indexed for MEDLINE]
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