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Design, synthesis and biological evaluation of new inhibitors of Bax/Bcl-xL interaction in cancer cells.

Abstract : We describe the synthesis of a series of new molecules containing phenol and triazoles moieties, compounds which have been evaluated for their ability to inhibit Bax/Bcl-xL interactions in cancer cells, by using BRET assays, and to induce cell death. Several derivatives exhibit a very promising activity, being more potent than the reference compounds acylpyrogallol A and ABT-737. These preliminary results demonstrate that derivatives of this family can be attractive to develop new molecules with potent anticancer activity.
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https://hal-univ-rennes1.archives-ouvertes.fr/hal-01116303
Contributor : Laurent Jonchère <>
Submitted on : Friday, February 13, 2015 - 9:31:54 AM
Last modification on : Saturday, July 11, 2020 - 3:16:37 AM

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Duc Duy Vo, Fabien Gautier, Sophie Barillé-Nion, Philippe Juin, Nicolas Levoin, et al.. Design, synthesis and biological evaluation of new inhibitors of Bax/Bcl-xL interaction in cancer cells.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2014, 24 (7), pp.1758-61. ⟨10.1016/j.bmcl.2014.02.035⟩. ⟨hal-01116303⟩

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