Abstract

AbstractA novel series of benzo[6,7]oxepino[4,3,2‐cd]indol‐1(2H)‐one derivatives were synthesized via a one‐pot aldol condensation and SNAr reaction by coupling indolin‐2‐ones with 2‐fluorobenzaldehydes. In addition, molecular docking studies of the designed compound 2 revealed strong hydrogen bonds in the hot binding pocket of Brd4. All compounds were evaluated for their enzymatic activity in Brd4 bromodomain inhibition.

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