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

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.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► synthesis of selected polyphenol derivatives which have been evaluated against Bax/Bcl-xL interaction. ► six of these derivatives exhibit activity comparable to ABT-737 to disrupt Bax/Bcl-xL interaction. ► the phenol at position 3 is important regarding Bax/Bcl-xL interaction.