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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Inhibition of Bfl-1 with N-aryl maleimides.

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.[1]

References

  1. Inhibition of Bfl-1 with N-aryl maleimides. Cashman, J.R., MacDonald, M., Ghirmai, S., Okolotowicz, K.J., Sergienko, E., Brown, B., Garcia, X., Zhai, D., Dahl, R., Reed, J.C. Bioorg. Med. Chem. Lett. (2010) [Pubmed]
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