Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction

Duc Duy Vo; Fabien Gautier; Philippe Juin; René Grée

doi:10.1016/j.ejmech.2012.02.036

Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction

Eur J Med Chem. 2012 May:51:286-93. doi: 10.1016/j.ejmech.2012.02.036. Epub 2012 Feb 25.

Authors

Duc Duy Vo¹, Fabien Gautier, Philippe Juin, René Grée

Affiliation

¹ Université de Rennes1, Laboratoire Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France.

PMID: 22425031
DOI: 10.1016/j.ejmech.2012.02.036

Abstract

This paper describes the synthesis of nine selected diaryl/heteroaryl-containing phenol and polyphenol derivatives which have been evaluated against Bax/Bcl-xL interaction in comparison with ABT-737. Using a BRET assay, six of these derivatives exhibit activity comparable to ABT-737 to disrupt Bax/Bcl-xL interaction. These preliminary results demonstrate that such polyphenol-derived molecules are attractive compounds regarding anticancer activity and that the phenol at position 3 is important regarding disruption of Bax/Bcl-xL interaction.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects
HeLa Cells
Humans
Polyphenols / chemistry*
Polyphenols / pharmacology*
Protein Binding / drug effects
Structure-Activity Relationship
bcl-2-Associated X Protein / metabolism*
bcl-X Protein / metabolism*

Substances

Antineoplastic Agents
Polyphenols
bcl-2-Associated X Protein
bcl-X Protein