Development of 3-acetylindole derivatives that selectively target BRPF1 as new inhibitors of receptor activator of NF-κB ligand (RANKL)-Induced osteoclastogenesis
Bioorganic & Medicinal Chemistry(2023)
摘要
•A series of 3-acetylindole derivatives were identified as selective BRPF1 inhibitors.•Compound 18 exhibited potent in vitro activity and no cytotoxicity toward osteoclast precursor cells.•Compound 18 impaired RANKL-induced differentiation osteoclasts and suppressed bone resorption through the NFATc1–c-fos pathway.•18 could serve as a tool compound to investigate the distinct biological functions of BRPF1 and a starting point for further research on drugs specifically targeting BRPF1.
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关键词
3-Acetylindole,Osteoclasts,RANKL,BRPF1
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