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.

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► 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.