Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands
Jing Fang1, Adwoa Akwabi-Ameyaw, Jonathan E Britton
1GlaxoSmithKline 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.
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