Cited by 15Cell death mechanisms and regulationSynthesis and biological activityComputational Drug Discovery Methods

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

Vo, Duc Duy, Gautier, Fabien, Juin, Philippe, Grée, René·2012·European Journal of Medicinal Chemistry

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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Crossref · 10.1016/j.ejmech.2012.02.036

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42 of 42 references verified0 citation errors · 0 not checkable

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Authors
Vo, D. D., Gautier, F., Juin, P., & Grée, R.
Affiliations
  • Centre National de la Recherche Scientifique (FR)
  • Inserm (FR)
Venue
European Journal of Medicinal Chemistry
Publisher
Elsevier BV
Published
2012-05
Volume
51
Pages
286-293
ISSN
0223-5234 (ISSN-L)
OpenAlex
W2079532359
Cited by
14
References
42
Citations by year
2021: 2 · 2018: 1 · 2017: 2 · 2016: 1 · 2015: 3 · 2014: 3 · 2013: 2
FWCI
1.03
Type
journal article
Language
en
Open access
closed
Locations
  • European Journal of Medicinal Chemistry (publishedVersion)
  • PubMed (publishedVersion)
  • HAL (submittedVersion)
Funders
  • Ligue Contre le Cancer
  • Servier
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cell death mechanisms and regulation
  • Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
  • Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
Keywords
structure-activity relationship, polyphenol derivatives, ABT-737, anticancer agents, apoptosis
MeSH terms
Antineoplastic Agents, HeLa Cells, Humans, Protein Binding, Structure-Activity Relationship, Apoptosis, bcl-X Protein, bcl-2-Associated X Protein, Polyphenols

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