Structure-activity relationship and bioactivity studies of neurotrophic -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 (−) trans -banglene is the active enantiomer. Assays performed with and without NGF prote...

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Veröffentlicht in:Organic & biomolecular chemistry 2022-03, Vol.2 (11), p.2187-2193
Hauptverfasser: Gohil, Khyati, Kazmi, M. Zain H, Williams, Florence J
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Zusammenfassung: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 (−) trans -banglene is the active enantiomer. Assays performed with and without NGF protein suggest that neurotrophic activity and potentiation of NGF activity by (−) trans -banglene might be distinct unassociated processes. Interestingly, (−) trans -banglene potentiation of NGF-induced neuritogenesis is unaffected by the presence of Erk1/2, Akt and Pkc inhibitors. The synthesis and bioactivity of neurotrophic banglenes and derivatives is described, establishing a structure-activity relationship which enables future mechanistic studies.
ISSN:1477-0520
1477-0539
DOI:10.1039/d2ob00016d