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Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2012

Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators.

Résumé

The synthesis of quinoline derivatives, designed to interact with Bcl-xL, and to inhibit its interaction with pro-apoptotic partners, is described and their biological effects investigated. We showed that 5 out of 28 synthetized compounds restored cell death of 3T3 cells overexpressing Bcl-xL following serum starvation. Active compounds were further characterized for their binding capacity to the anti-apoptotic member of the Bcl-2 family, Bcl-xL as well as Bcl-2, Bfl-1 and Mcl-1, and for their pro-apoptotic activities toward lymphoid tumor cells and peripheral blood mononuclear cells. Altogether our results indicate that dimeric, rather than trimeric quinoline derivatives, represent a new attractive class of BH3 mimetics for cancer therapy.
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Dates et versions

hal-00786361 , version 1 (08-02-2013)

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  • HAL Id : hal-00786361 , version 1

Citer

Emmanuelle Saugues, Anne-Laure Debaud, Fabrice Anizon, Nathalie Bonnefoy, Pascale Moreau. Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators.. European Journal of Medicinal Chemistry, 2012, 57, pp.112-125. ⟨hal-00786361⟩
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