Synthesis and biological activities of new di- and trimeric quinoline derivatives
| Autor: | Sidonie Broch, Pascale Moreau, Anne-Laure Debaud, Hélène Henon, Marie-Laure Fogeron, Nathalie Bonnefoy-Berard, Fabrice Anizon |
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| Rok vydání: | 2010 |
| Předmět: |
Models
Molecular Stereochemistry Clinical Biochemistry bcl-X Protein Pharmaceutical Science Apoptosis Trimer Stereoisomerism Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Structure–activity relationship Binding site Molecular Biology Binding Sites Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Quinoline Biological activity Recombinant Proteins Proto-Oncogene Proteins c-bcl-2 Helix Quinolines Molecular Medicine Dimerization |
| Zdroj: | Bioorganic & Medicinal Chemistry. 18:7132-7143 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2010.07.029 |
| Popis: | 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-x(L)/Bak, Bcl-x(L)/Bax and Bcl-x(L)/Bid interactions with IC(50) values around 25 μM. |
| Databáze: | OpenAIRE |
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