100728-74-3Relevant academic research and scientific papers
Structure-activity relationship study of N N6-benzoyladenine-type BRD4 inhibitors and their effects on cell differentiation and TNF-α production
Amemiya, Seika,Yamaguchi, Takao,Sakai, Taki,Hashimoto, Yuichi,Noguchi-Yachide, Tomomi
, p. 1378 - 1383 (2016)
Bromodomains are epigenetic 'readers' of histone acetylation. The first potent bromodomain and extra-terminal domain (BET) inhibitors, (+)-JQ1 and I-BET762 (also known as GSK525762), were reported in 2010. Some BET inhibitors are already under clinical trial for the treatment of cancers, but so far, only a few chemical scaffolds are available. We have reported potent N N6-benzoyladenine-based inhibitors of BRD4, a BET family member that serves as a key mediator of transcriptional elongation. Here we present an analysis of the structure-activity relationships of these inhibitors. Among the compounds examined, 20, 28 and 29 enhanced all-trans retinoic acid (ATRA)-induced HL-60 cell differentiation and inhibited tumor necrosis factor (TNF)-α production by THP-1 cells.
Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors
Noguchi-Yachide, Tomomi,Sakai, Taki,Hashimoto, Yuichi,Yamaguchi, Takao
, p. 953 - 959 (2015/03/04)
Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers that bind to acetylated lysines in histones. Among them, BRD4 is a candidate target molecule of therapeutic agents for diverse diseases, including cancer and inflammatory disease.
