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

Eur J Med Chem. 2012 May:51:286-93. doi: 10.1016/j.ejmech.2012.02.036. Epub 2012 Feb 25.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • HeLa Cells
  • Humans
  • Polyphenols / chemistry*
  • Polyphenols / pharmacology*
  • Protein Binding / drug effects
  • Structure-Activity Relationship
  • bcl-2-Associated X Protein / metabolism*
  • bcl-X Protein / metabolism*

Substances

  • Antineoplastic Agents
  • Polyphenols
  • bcl-2-Associated X Protein
  • bcl-X Protein