[摘要]: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. (C) 2008 Elsevier Ltd. All rights reserved.