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Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2010

Synthesis and biological activities of new di- and trimeric quinoline derivatives

Résumé

The synthesis of non-peptidic helix mimetics based on a trimeric quinoline scaffold is described. The ability of these new compounds, as well as their synthetic dimeric intermediates, to bind to various members of the Bcl-2 protein anti-apoptotic group is also evaluated. The most interesting derivative of this new series (compound A) inhibited Bcl-xL/Bak, Bcl-xL/Bax and Bcl-xL/Bid interactions with IC50 values around 25 μM.
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hal-00530608 , version 1 (29-10-2010)

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  • HAL Id : hal-00530608 , version 1

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Sidonie Broch, Hélène Henon, Anne-Laure Debaud, Marie-Laure Fogeron, Nathalie Bonnefoy-Bérard, et al.. Synthesis and biological activities of new di- and trimeric quinoline derivatives. Bioorganic and Medicinal Chemistry, 2010, 18, pp.7132-7143. ⟨hal-00530608⟩
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