Nian, Si-Yun; Wang, Guo-Ping; Jiang, Zheng-Li; Xiao, Ying; Huang, Mo-Han; Zhou, Yi-Huan; Tan, Xiang-Duan published the artcile< Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists>, Recommanded Product: 4-(2-Bromoacetyl)benzoic acid, the main research area is hypercholesterolemia farnesoid X receptor antagonist SIPI7623; FXR antagonists; Guggulsterone; Molecular docking; SIPI-7623; Structure activity relationship.
Most of reported steroidal FXR antagonists are restricted due to low potency. We described the design and synthesis of novel nonsteroidal scaffold SIPI-7623 derivatives as FXR antagonists. The most potent compound A-11 (IC50 = 7.8 ± 1.1 μM) showed better activity compared to SIPI-7623 (IC50 = 40.8 ± 1.7 μM) and guggulsterone (IC50 = 45.9 ± 1.1 μM). Docking of A-11 in FXR′s ligand-binding domain was also studied.
Molecular Diversity published new progress about Drug design. 20099-90-5 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO3, Recommanded Product: 4-(2-Bromoacetyl)benzoic acid.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary