Structure-activity relationship and bioactivity studies of neurotrophic trans -banglene

The synthesis and bioactivity of neurotrophic banglenes and derivatives is described, establishing a structure-activity relationship which enables future mechanistic studies. Neuritogenesis assays indicate that (-) -banglene is the active enantiomer. Assays performed with and without NGF protein sug...

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Bibliographic Details
Published in:Organic & biomolecular chemistry 2022-03, Vol.20 (11), p.2187-2193
Main Authors: Gohil, Khyati, Kazmi, M Zain H, Williams, Florence J
Format: Article
Language:English
Subjects:
AKT protein
Animals
Axonogenesis
Biological activity
Enantiomers
Molecular Structure
Nerve growth factor
Nerve Growth Factor - chemistry
Nerve Growth Factor - pharmacology
Neurites - drug effects
Neurites - metabolism
PC12 Cells
Potentiation
Protein kinase C
Rats
Stereoisomerism
Structure-Activity Relationship
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Summary:The synthesis and bioactivity of neurotrophic banglenes and derivatives is described, establishing a structure-activity relationship which enables future mechanistic studies. Neuritogenesis assays indicate that (-) -banglene is the active enantiomer. Assays performed with and without NGF protein suggest that neurotrophic activity and potentiation of NGF activity by (-) -banglene might be distinct unassociated processes. Interestingly, (-) -banglene potentiation of NGF-induced neuritogenesis is unaffected by the presence of Erk1/2, Akt and Pkc inhibitors.
ISSN:1477-0520
1477-0539
1477-0539
DOI:10.1039/d2ob00016d