Preliminary Studies on the Activity of Mixed Polyphenol-Heterocyclic Systems Against B16-F10 Melanoma Cancer Cells - Archive ouverte HAL Access content directly
Journal Articles Medicinal Chemistry Year : 2016

Preliminary Studies on the Activity of Mixed Polyphenol-Heterocyclic Systems Against B16-F10 Melanoma Cancer Cells

(1) , (1) , (1) , (2, 3, 4) , (3) , (3) , (5) , (1) , (1)
1
2
3
4
5

Abstract

The Bcl-2 family includes 26 proteins involved in apoptosis. Cancer cells can develop the ability to avoid apop-tosis through the upregulation and/or down regulation of such proteins Bax, Bcl-xL or Mcl-1, especially during chemore-sistance progress. These proteins engaged in a network of dynamic interactions that control apoptosis triggering have become attractive therapeutic targets in cancers including melanoma. Among them, the Bax/Bcl-xL interaction appears critical in maintaining mitochondria integrity. Therefore a series of mixed polyphenol-heterocyclic molecules, were rationally designed by molecular docking as Bax/Bcl-xL inhibitors. It has been screened against B16-F10 melanoma cancer cells for a preliminary investigation of their cytotoxicity. All these compounds exhibited a significant cytotoxicity against these cancer cells, in the 0.3-6 μM range. A pyrazole-type molecule, which had a submicromolar IC 50 value with an excellent selectivity index (14), is the most promising derivative for further development.
Embargoed file
Embargoed file
Ne sera jamais visible
Loading...

Dates and versions

inserm-01406309 , version 1 (01-12-2016)

Identifiers

  • HAL Id : inserm-01406309 , version 1
  • PUBMED : 26825069

Cite

Duc Duy Vo, Isabelle Rouaud, Françoise Lohézic-Le Dévéhat, Fabien Gautier, Sophie Barillé-Nion, et al.. Preliminary Studies on the Activity of Mixed Polyphenol-Heterocyclic Systems Against B16-F10 Melanoma Cancer Cells. Medicinal Chemistry, 2016. ⟨inserm-01406309⟩
86 View
0 Download

Altmetric

Share

Gmail Facebook Twitter LinkedIn More