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Bioorg Med Chem Lett. 2008 Sep 15;18(18):5075-7. doi: 10.1016/j.bmcl.2008.07.121. Epub 2008 Aug 5.

Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands.

Author information

1
GlaxoSmithKline Research, 5 Moore Drive, Research Triangle Park, NC 27709, USA. jing.m.fang@gsk.com

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.

PMID:
18722117
DOI:
10.1016/j.bmcl.2008.07.121
[Indexed for MEDLINE]

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