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

Université de Rennes1, Laboratoire Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France.
European journal of medicinal chemistry (Impact Factor: 3.27). 02/2012; 51:286-93. DOI: 10.1016/j.ejmech.2012.02.036
Source: PubMed

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.