ArticleBioorganic & medicinal chemistry letters2009
(+/-)-Nantenine analogs as antagonists at human 5-HT(2A) receptors: C1 and flexible congeners.
Article in Bioorganic & medicinal chemistry letters, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
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- Total Synthesis of Aporphine Alkaloids via Photocatalytic Oxidative Phenol Coupling and Biological Evaluation at the Serotonin 5-HTJournal of medicinal chemistry · 2025Article
- Total Synthesis of the Racemate of Laurolitsine.Molecules (Basel, Switzerland) · 2024Article
- Structure-activity profiling of alkaloid natural product pharmacophores against a Schistosoma serotonin receptor.International journal for parasitology. Drugs and drug resistance · 2018Article
- Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HTMedChemComm · 2018Article
- Article
- Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.Bioorganic & medicinal chemistry letters · 2015Article
- C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.Bioorganic & medicinal chemistry letters · 2015Article
- Evaluation of structural effects on 5-HT(2A) receptor antagonism by aporphines: identification of a new aporphine with 5-HT(2A) antagonist activity.Bioorganic & medicinal chemistry letters · 2014Article
- Facile synthesis of 4,5,6a,7-tetrahydrodibenzo[de,g]chromene heterocycles and their transformation to phenanthrene alkaloids.Tetrahedron · 2013Article
- A New Route to Azafluoranthene Natural Products via Direct Arylation.European journal of organic chemistry · 2013Article
- New aporphinoid 5-HT2A and α1A antagonists via structural manipulations of nantenine.Bioorganic & medicinal chemistry · 2011Article
- Cytotoxicity of aporphines in human colon cancer cell lines HCT-116 and Caco-2: an SAR study.Bioorganic & medicinal chemistry letters · 2011Article
- Nantenine as an acetylcholinesterase inhibitor: SAR, enzyme kinetics and molecular modeling investigations.Journal of enzyme inhibition and medicinal chemistry · 2011Article
- Synthesis of C-Homoaporphines via Microwave-Assisted Direct Arylation.Tetrahedron · 2011Article
- Affinity of aporphines for the human 5-HT2A receptor: insights from homology modeling and molecular docking studies.Bioorganic & medicinal chemistry · 2010Article
- Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.Bioorganic & medicinal chemistry letters · 2010Article
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5 authors.
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Abstract
C1 and flexible analogs of (+/-)-nantenine were synthesized and evaluated for antagonist activity at human 5-HT(2A) receptors in a calcium mobilization assay. This work has resulted in the identification of the most potent 5-HT(2A) antagonist known based on an aporphine. Our results also suggest that the C1 position may be a key site for increasing 5-HT(2A) antagonist activity in this compound series. In addition, the structural rigidity of the aporphine core appears to be required for nantenine to function as a 5-HT(2A) antagonist.
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