Synthesis and biological activity of (±)-7,3',4'-trihydroxyhomoisoflavan and its analogs.
Acetylcholinesterase
/ metabolism
Animals
Cholinesterase Inhibitors
/ chemical synthesis
Dose-Response Relationship, Drug
Dracaena
/ chemistry
Humans
Molecular Docking Simulation
Molecular Structure
Nerve Growth Factors
/ metabolism
Neurites
/ drug effects
PC12 Cells
Rats
Structure-Activity Relationship
AChE inhibitory activity
Dracaena cambodiana
Dragon’s blood
Homoisoflavan
Neurite outgrowth promoting activity
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 01 2021
01 01 2021
Historique:
received:
14
09
2020
revised:
26
10
2020
accepted:
01
11
2020
pubmed:
9
11
2020
medline:
23
7
2021
entrez:
8
11
2020
Statut:
ppublish
Résumé
Acetylcholinesterase (AChE) inhibitors and neurite outgrowth promoters are thought to alleviate the symptoms of degenerative brain disorders, such as Alzheimer's disease. We designed and synthesized a series of homoisoflavonoids based on the structure of natural homoisoflavan isolated from Dracaena cambodiana dragon's blood. The homoisoflavonoids were then evaluated as AChE inhibitors and neurite outgrowth promoters. The catechol structure of the homoisoflavan B rings was important for AChE inhibition, and some of the homoisoflavonoids significantly promoted neurite outgrowth induced by nerve growth factor (NGF).
Identifiants
pubmed: 33161123
pii: S0960-894X(20)30785-X
doi: 10.1016/j.bmcl.2020.127674
pii:
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Nerve Growth Factors
0
Acetylcholinesterase
EC 3.1.1.7
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
127674Informations de copyright
Copyright © 2020. Published by Elsevier Ltd.