Abstract
A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. Several of these compounds bearing a C6-OH group were shown to be high affinity ligands. All compounds had similar ERalpha and ERbeta binding affinity ranging from micromolar to low nanomolar.
MeSH terms
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Combinatorial Chemistry Techniques
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Estrogen Receptor Modulators / metabolism
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Estrogen Receptor alpha / metabolism
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Estrogen Receptor beta / metabolism
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Female
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Humans
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Ligands
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Molecular Structure
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Naphthalenes / chemical synthesis*
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Naphthalenes / chemistry
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Naphthalenes / pharmacology*
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Receptors, Estrogen / agonists*
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Selective Estrogen Receptor Modulators / metabolism
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Structure-Activity Relationship
Substances
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Estrogen Receptor Modulators
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Ligands
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Naphthalenes
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Receptors, Estrogen
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Selective Estrogen Receptor Modulators