| Title : Synthesis and biological evaluation of genistein-O-alkylamine derivatives as potential multifunctional anti-Alzheimer agents - Hong_2019_Chem.Biol.Drug.Des_93_188 |
| Author(s) : Hong C , Guo HY , Chen S , Lv JW , Zhang X , Yang YC , Huang K , Zhang YJ , Tian ZY , Luo W , Chen YP |
| Ref : Chemical Biology Drug Des , 93 :188 , 2019 |
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Abstract :
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 inhibition to AChE with an IC50 value (0.034 muM) much lower than that of rivastigmine (6.53 muM). A Lineweaver-Burk plot and molecular modeling study showed that compound 5a targeted both the catalytic active site and the peripheral anionic site of AChE. These compounds also showed potent peroxy scavenging activity and metal-chelating ability. The compounds did not show obvious effect on HepG2 and PC12 cell viability at the concentration of 100 muM. Therefore, these genistein derivatives can be utilized as multifunctional agents for the treatment of AD. |
| PubMedSearch : Hong_2019_Chem.Biol.Drug.Des_93_188 |
| PubMedID: 30299583 |
Hong C, Guo HY, Chen S, Lv JW, Zhang X, Yang YC, Huang K, Zhang YJ, Tian ZY, Luo W, Chen YP (2019)
Synthesis and biological evaluation of genistein-O-alkylamine derivatives as potential multifunctional anti-Alzheimer agents
Chemical Biology Drug Des
93 :188
Hong C, Guo HY, Chen S, Lv JW, Zhang X, Yang YC, Huang K, Zhang YJ, Tian ZY, Luo W, Chen YP (2019)
Chemical Biology Drug Des
93 :188