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Bioorg Med Chem Lett
; 18(18): 5075-7, 2008 Sep 15.
Article
in English
| MEDLINE
| ID: mdl-18722117
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.