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

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.
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Medicinal Chemistry, Bentham Science Publishers, 2016
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  • HAL Id : inserm-01406309, version 1

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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, Bentham Science Publishers, 2016. 〈inserm-01406309〉

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