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ID: ALA1250523

Journal: Bioorg Med Chem

Title: Synthesis and biological activities of new di- and trimeric quinoline derivatives.

Authors: Broch S, Hénon H, Debaud AL, Fogeron ML, Bonnefoy-Bérard N, Anizon F, Moreau P.

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-x(L)/Bak, Bcl-x(L)/Bax and Bcl-x(L)/Bid interactions with IC(50) values around 25 μM.

CiteXplore: 20800501

DOI: 10.1016/j.bmc.2010.07.029