Inhibition of Bfl-1 with N-aryl maleimides

…, E Sergienko, B Brown, X Garcia, D Zhai, R Dahl…

Index: Cashman, John R.; MacDonald, Mary; Ghirmai, Senait; Okolotowicz, Karl J.; Sergienko, Eduard; Brown, Brock; Garcia, Xochella; Zhai, Dayong; Dahl, Russell; Reed, John C. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6560 - 6564

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Citation Number: 14

Abstract

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 ...