145370-50-9Relevant academic research and scientific papers
Cleavage of methyl ethers of flavones by chloroaluminate ionic liquid
Liu, Tao,Hu, Yongzhou
, p. 3209 - 3218 (2004)
A new o-demethylation method of a series of mono-, di-, trimethoxy-flavones using a chloroaluminate ionic liquid - [BMIM] [Al2Cl7] in dichloromethane is described. The desired products were obtained in moderate to good yields.
Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists
Zhang, Guoning,Liu, Shuainan,Tan, Wenjuan,Verma, Ruchi,Chen, Yuan,Sun, Deyang,Huan, Yi,Jiang, Qian,Wang, Xing,Wang, Na,Xu, Yang,Wong, Chiwai,Shen, Zhufang,Deng, Ruitang,Liu, Jinsong,Zhang, Yanqiao,Fang, Weishuo
, p. 303 - 309 (2017/03/01)
Farnesoid X receptor (FXR), a nuclear receptor mainly distributed in liver and intestine, has been regarded as a potential target for the treatment of various metabolic diseases, cancer and infectious diseases related to liver. Starting from two previously identified chalcone-based FXR antagonists, we tried to increase the activity through the design and synthesis of a library containing chalcones, flavones and chromenes, based on substitution manipulation and conformation (ring closure) restriction strategy. Many chalcones and four chromenes were identified as microM potent FXR antagonists, among which chromene 11c significantly decreased the plasma and hepatic triglyceride level in KKay mice.
Design, synthesis and evaluation of novel 7-aminoalkyl-substituted flavonoid derivatives with improved cholinesterase inhibitory activities
Luo, Wen,Chen, Ying,Wang, Ting,Hong, Chen,Chang, Li-Ping,Chang, Cong-Cong,Yang, Ya-Cheng,Xie, Song-Qiang,Wang, Chao-Jie
, p. 672 - 680 (2016/02/09)
A novel series of 7-aminoalkyl-substituted flavonoid derivatives 5a-5r were designed, synthesized and evaluated as potential cholinesterase inhibitors. The results showed that most of the synthesized compounds exhibited potent acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities at the micromolar range. Compound 2-(naphthalen-1-yl)-7-(8-(pyrrolidin-1-yl)octyloxy)-4H-chromen-4-one (5q) showed the best inhibitory activity (IC50, 0.64 μM for AChE and 0.42 μM for BChE) which were better than our previously reported compounds and the commercially available cholinergic agent Rivastigmine. The results from a Lineweaver-Burk plot indicated a mixed-type inhibition for compound 5q with AChE and BChE. Furthermore, molecular modeling study showed that 5q targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, these compounds (5a-5r) did not affect PC12 and HepG2 cell viability at the concentration of 10 μM. Consequently, these flavonoid derivatives should be further investigated as multipotent agents for the treatment of Alzheimer's disease.
