ArticleChemical biology & drug design2014
Aporphinoid antagonists of 5-HT2A receptors: further evaluation of ring A substituents and the size of ring C.
Article in Chemical biology & drug design, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 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
- Mechanism Exploration of Arylpiperazine Derivatives Targeting the 5-HTMolecules (Basel, Switzerland) · 2017Article
- 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
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Authors and funding
4 authors.
Funding
Abstract
A series of ring A-modified analogs of nantenine as well as structural variants in ring C were synthesized and evaluated for antagonist activity at 5-HT2A and α1A receptors. Halogenation improves 5-HT2A antagonist potency in molecules containing a C1 methoxyl/C2 methoxyl or C1 methoxyl/C2 hydroxyl moiety. Bromination or iodination (but not chlorination) with the latter moiety also significantly increased α1A antagonist potency. Homologation or contraction of ring C adversely affected antagonist activity at both receptors, implying that a six-membered ring C motif is beneficial for high antagonist potency at both receptors. Molecular docking studies suggest that the improved antagonist activity (by virtue of improved affinity) of C3-halogenated aporphines in this study is attributable to favorable interactions with the C3 halogen and F339 and/or F340.
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