1343498-63-4Relevant academic research and scientific papers
Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists
Nian, Si-Yun,Wang, Guo-Ping,Jiang, Zheng-Li,Xiao, Ying,Huang, Mo-Han,Zhou, Yi-Huan,Tan, Xiang-Duan
, p. 1 - 15 (2018/07/13)
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.
Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism
De Filippis, Barbara,Giancristofaro, Antonella,Ammazzalorso, Alessandra,D'Angelo, Alessandra,Fantacuzzi, Marialuigia,Giampietro, Letizia,MacCallini, Cristina,Petruzzelli, Michele,Amoroso, Rosa
, p. 5218 - 5224 (2011/11/29)
A new series of gemfibrozil analogues conjugated with α-asarone, trans-stilbene, chalcone, and their bioisosteric modifications were synthesized and evaluated to develop PPARα agonists. In this attempt, we have removed the methyls on the phenyl ring of gemfibrozil and introduced the above scaffolds in para position synthesizing two series of derivatives, keeping the dimethylpentanoic skeleton of gemfibrozil unaltered or demethylated. Four compounds exhibited good activation of the PPARα receptor and were also screened for their activity on PPARα-regulated gene CPT1A.
