1204747-90-9Relevant articles and documents
Synthesis and biological evaluation of genistein-IR783 conjugate: Cancer cell targeted delivery in MCF-7 for superior anti-cancer therapy
Guan, Yang,Zhang, Yi,Zou, Juan,Huang, Li-Ping,Chordia, Mahendra D.,Yue, Wei,Wu, Jin-Jun,Pan, Dong-Feng
, (2019)
The flavonoid-based natural product genistein is a biologically active compound possessing promising anti-oxidant and anti-cancer properties. Poor pharmacokinetics along with low potency limit however the therapeutic application of genistein in cancer the
Synthesis and biological evaluation of genistein-O-alkylamine derivatives as potential multifunctional anti-Alzheimer agents
Hong, Chen,Guo, Hui-yan,Chen, Shuai,Lv, Jian-wu,Zhang, Xin,Yang, Ya-cheng,Huang, Kang,Zhang, Yi-juan,Tian, Zhi-yong,Luo, Wen,Chen, Yi-ping
, p. 188 - 200 (2018/10/26)
A series of genistein derivatives were synthesized and evaluated as multifunctional anti-Alzheimer agents. The results showed that these derivatives had significant acetylcholinesterase (AChE) inhibitory activity; compound 5a exhibited the strongest inhib
Flavonoid compound targeting tumor cells and preparation method of flavonoid compound
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Paragraph 0023; 0024; 0025, (2016/12/16)
The invention belongs to the field of organic chemistry and relates to a flavonoid compound targeting tumor cells. A chemical structural formula of the flavonoid compound is as shown in a formula (I). Isoflavone and IR783 are reacted under the action of N
Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease
Qiang, Xiaoming,Sang, Zhipei,Yuan, Wen,Li, Yan,Liu, Qiang,Bai, Ping,Shi, Yikun,Ang, Wei,Tan, Zhenghuai,Deng, Yong
, p. 314 - 331 (2014/03/21)
A series of genistein derivatives with carbon spacer-linked alkylbenzylamines were designed, synthesized and tested as multifunctional agents for the treatment of Alzheimer's disease (AD). The results showed that most of these compounds exhibited good acetylcholinesterase (AChE) inhibitory activity, with moderate-to-good anti-oxidative activity. Specifically, compounds 10b, 19d and 25d exhibited significant inhibition of β-amyloid (Aβ) aggregation and exhibited metal chelating properties. In particular, 25d inhibited: self-induced Aβ1-42 aggregation, Cu 2+-induced Aβ1-42 aggregation, and human AChE-induced Aβ1-40 aggregation by 35%, 77.8%, and 36.2%, respectively. Moreover, both kinetic analysis of AChE inhibition and the molecular modeling study suggested that 25d binds simultaneously to catalytic active site and peripheral anionic site of AChE. More importantly, compound 25d disassembled the well-structured Aβ fibrils generated by Cu2+-induced Aβ aggregation by 72.1%. Furthermore, the step-down passive avoidance test showed this compound significantly reversed scopolamine-induced memory deficit in mice. These results suggest that 25d may be a promising multifunctional agent for AD treatment.
Novel phenoxyalkylcarboxylic acid derivatives as hypolipidaemic agents
Li, Wei,Jia, Hao-Yan,He, Xin-Hua,Shi, Wei-Guo,Zhong, Bo-Hua
experimental part, p. 311 - 318 (2012/07/02)
Novel phenoxyalkylcarboxylic acid derivatives based on the natural scaffolds, flavonoids, or resveratrol were designed, synthesized, and evaluated for hypolipidaemic activity. Among the compounds, 30b lowered the triglycerides by 48.5% (P0.05) and total cholesterol by 44.2% (P0.05), respectively, and was more effective than the reference drug fenofibric acid in a Triton WR-1339-induced hyperlipidaemic mice model orally (300mg/kg body weight). 30b also showed 59.4% triglycerides lowering in an alloxan-induced diabetic mice model orally (150mg/kg body weight). Receptor docking studies revealed that compound 30b could interact with the amino acid residues in the ligand-binding domain essential for the activation of the PPARα. The results indicate that resveratrol should be a better scaffold to derive a new class of hypolipidaemic agents in comparison with a flavonoid scaffold.