Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors

A series of novel derivatives 4-9 and 11-54 bearing with benzo[cd]indol-2(1H)-one scaffold have been designed and synthesized through structure-based optimization on a lead BRD4 inhibitor 1. Compounds 23, 24, 28 and 44 are the most potential BRD4 inhibitors and compounds 23 and 44 exhibit significantly inhibitory activities against MLL-rearranged MV4-11 cells proliferation.216