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

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.