Discovery of Benzo[<i>cd</i>]indol-2(1<i>H</i>)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation
The discovery of inhibitors of bromodomain and extra terminal domain (BET) has achieved great progress, and at least seven inhibitors have progressed into clinical trials for the treatment of cancer or inflammatory diseases. Here, we describe the identification, optimization, and evaluation of benzo[cd]indol-2(1H)-one containing compounds as a new class of BET bromodomain inhibitors, starting from
[EN] 2-OXO-1,2-DIHYDROBENZO[CD]INDOLE-6-SULFONAMIDE COMPOUND AND COMPOSITION AND USE THEREOF<br/>[FR] COMPOSÉ 2-OXO-1,2-DIHYDROBENZO[CD]INDOLE-6-SULFONAMIDE ET COMPOSITION ET UTILISATION CORRESPONDANTES<br/>[ZH] 2-氧代-1,2-二氢苯并[cd]吲哚-6-磺酰胺类化合物及其组合物和应用