399-95-1Relevant articles and documents
A potent free fatty acid receptor 1 agonist with a glucose-dependent antihyperglycemic effect
Wang, Xuekun,Xu, Yurui,Feng, Shujun,Huang, Xinyu,Meng, Xia,Chen, Jiao,Guo, Leilei,Ge, Junliang,Zhang, Jikang,Chen, Jianmei,Cheng, Li,Gu, Kai,Zhang, Yu,Jiang, Qing,Ning, Xinghai
, p. 8975 - 8978 (2019)
We present a novel free fatty acid receptor 1 (FFA1) agonist, named PAFA, with a strong agonist potency (EC50 = 6.04 nM) and good serum stability. PAFA significantly stimulates insulin secretion in INS-1 cells in a glucose-dependent manner and exhibits high antihyperglycemic effects in db/db mice without adverse effects.
Regorafenib analogues and their ferrocenic counterparts: Synthesis and biological evaluation
Wilde, Myron,Arzur, Danielle,Baratte, Blandine,Lefebvre, Dorian,Robert, Thomas,Roisnel, Thierry,Le Jossic-Corcos, Catherine,Bach, Stéphane,Corcos, Laurent,Erb, William
supporting information, p. 19723 - 19733 (2020/12/04)
Approved by the FDA in 2012, regorafenib is one of the last chance treatments for colorectal cancer. While various analogues have already been prepared, ferrocenic derivatives have never been evaluated. In this study, we prepared various ferrocene-containing derivatives of regorafenib and recorded their biological activity in kinase and cellular assays. This led to the identification of a squaramide derivative which shows a good cellular activity and three ferrocene analogues with promising activity in both kinase and cellular assays. This journal is
A process for preparing auspicious standard phinney intermediates
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Paragraph 0007; 0014-0015; 0018-0019; 0024; 0029; 0034, (2019/05/06)
The invention discloses a method for preparing a regorafenib intermediate; a compound represented by the formula II and a compound represented by the formula III are subjected to three stages of a step A, a step B and a step C, intermediates of all the stages are not separated, and thus the regorafenib intermediate I is prepared. According to the method, the intermediates of all the steps are not separated, post-treatment procedures are reduced, the process operational flow is saved, the solvent recovery and utilization efficiency is improved, pollution emissions and energy consumption are reduced, the requirements on green chemical process are met, and the method is suitable for industrialized production.