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

Autor: Fang J; GlaxoSmithKline Research, 5 Moore Drive, Research Triangle Park, NC 27709, USA. jing.m.fang@gsk.com, Akwabi-Ameyaw A, Britton JE, Katamreddy SR, Navas F 3rd, Miller AB, Williams SP, Gray DW, Orband-Miller LA, Shearin J, Heyer D
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Sep 15; Vol. 18 (18), pp. 5075-7. Date of Electronic Publication: 2008 Aug 05.
DOI: 10.1016/j.bmcl.2008.07.121
Abstrakt: 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.
Databáze: MEDLINE