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Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands

Journal Article · · Bioorg. Med. Chem. Lett.

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 ER{alpha} and ER{beta} binding affinity ranging from micromolar to low nanomolar.

Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
USDOE
OSTI ID:
1007104
Journal Information:
Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (18) ; 09, 2008 Vol. 18; ISSN 0960-894X
Country of Publication:
United States
Language:
ENGLISH

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