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

…, AL Debaud, ML Fogeron, N Bonnefoy-Bérard…

文献索引：Broch, Sidonie; Heenon, Helne; Debaud, Anne-Laure; Fogeron, Marie-Laure; Bonnefoy-Berard, Nathalie; Anizon, Fabrice; Moreau, Pascale Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 19 p. 7132 - 7143

全文：HTML全文

被引用次数: 13

摘要

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 25μM.