448199-64-2Relevant articles and documents
Inhibition of Bfl-1 with N-aryl maleimides
Cashman, John R.,MacDonald, Mary,Ghirmai, Senait,Okolotowicz, Karl J.,Sergienko, Eduard,Brown, Brock,Garcia, Xochella,Zhai, Dayong,Dahl, Russell,Reed, John C.
supporting information; experimental part, p. 6560 - 6564 (2010/12/24)
High-throughput screening of 66,000 compounds using competitive binding of peptides comprising the BH3 domain to anti-apoptotic Bfl-1 led to the identification of 14 validated 'hits' as inhibitors of Bfl-1. N-Aryl maleimide 1 was among the validated 'hits'. A chemical library encompassing over 280 analogs of 1 was prepared following a two-step synthesis. Structure-activity studies for inhibition of Bfl-1 by analogs of N-aryl maleimide 1 revealed a preference for electron-withdrawing substituents in the N-aryl ring and hydrophilic amines appended to the maleimide core. Inhibitors of Bfl-1 are potential development candidates for anti-cancer therapeutics.
