title: Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction.
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.
authors.affiliation: Université de Rennes1, Laboratoire Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France.
authors.forename: Duc Duy
authors.initials: DD
authors.lastname: Vo
authors.forename: Fabien
authors.initials: F
authors.lastname: Gautier
authors.forename: Philippe
authors.initials: P
authors.lastname: Juin
authors.forename: René
authors.initials: R
authors.lastname: Grée
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D059808:Polyphenols / Q000737:chemistry* / Q000494:pharmacology*; D011485:Protein Binding / Q000187:drug effects; D013329:Structure-Activity Relationship; D051028:bcl-2-Associated X Protein / Q000378:metabolism*; D051020:bcl-X Protein / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D059808:Polyphenols; D051028:bcl-2-Associated X Protein; D051020:bcl-X Protein