Synthesis and biological activities of new di- and trimeric quinoline derivatives |
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| Authors: | Sidonie Broch Hélène Hénon Anne-Laure Debaud Marie-Laure Fogeron Nathalie Bonnefoy-Bérard Fabrice Anizon Pascale Moreau |
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| Affiliation: | 1. Clermont Université, Université Blaise Pascal, SEESIB, BP 10448, F-63000 Clermont-Ferrand, France;2. CNRS, UMR 6504, SEESIB, F-63177 Aubière, France;3. Université de Lyon, France;4. Inserm, U851, 21 Avenue Tony Garnier, Lyon F-69007, France;5. Université Lyon 1, IFR128, France |
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| Abstract: | 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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