Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction. - Archive ouverte HAL Access content directly
Journal Articles European Journal of Medicinal Chemistry Year : 2012

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

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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.
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hal-00841554 , version 1 (05-07-2013)

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Duc Duy Vo, Fabien Gautier, Philippe Juin, René Grée. Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction.. European Journal of Medicinal Chemistry, 2012, 51, pp.286-93. ⟨10.1016/j.ejmech.2012.02.036⟩. ⟨hal-00841554⟩
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