ArticleBioorganic & medicinal chemistry letters2015
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.
Article in Bioorganic & medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed.
- Regioselective Synthesis of 9‑ACS omega · 2026Article
- Total Synthesis of Aporphine Alkaloids via Photocatalytic Oxidative Phenol Coupling and Biological Evaluation at the Serotonin 5-HTJournal of medicinal chemistry · 2025Article
- Biological Potential of Oxoglaucine in Medicine for the Treatment of Human Disorders: An Update on Pharmacological Activities and Related Molecular Mechanism.Recent advances in anti-infective drug discovery · 2025Review
- Identification of C10 nitrogen-containing aporphines with dopamine DBioorganic & medicinal chemistry letters · 2020Article
- Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HTMedChemComm · 2018Article
- Pharmacological profiling an abundantly expressed schistosome serotonergic GPCR identifies nuciferine as a potent antagonist.International journal for parasitology. Drugs and drug resistance · 2016Article
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Authors and funding
5 authors.
Funding
Abstract
A series of C1 aporphine analogs related to compound 5 and that contain substituted allylic, alkynyl, nitrile, ester and benzyl groups was synthesized and evaluated for affinity at h5HT2A and α1A receptors in functional activity assays that measure calcium release. The presence of branched allylic substituent groups diminished affinity for the h5HT2A receptor. Likewise, the alkynyl, nitrile and ester derivatives evaluated displayed lower 5-HT2A receptor affinity as compared to 5. Hydrophobic, steric and electronic effects impact the affinity of p-substituted benzyl derivatives 8i-8k but in different ways. High hydrophobicity and size favor 5-HT2A affinity whereas, high electronegativity disfavors 5-HT2A affinity. p-Bromobenzyl analog 8k was identified as a 5-HT2A receptor selective ligand, with the highest 5-HT2A receptor affinity of any aporphine known to date. Most of the other analogs were selective for the 5-HT2A versus the α1A receptor. ChemScore binding energies from docking studies correlated qualitatively with the observed trends in affinity for 8i-8k, although the binding energies were not well differentiated quantitatively.
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