| 18722117 |
Fang J, Akwabi-Ameyaw A, Britton JE, Katamreddy SR, Navas F 3rd, Miller AB, Williams SP, Gray DW, Orband-Miller LA, Shearin J, Heyer D: Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands. . Bioorg Med Chem Lett. 2008 Sep 15;18(18):5075-7. Epub 2008 Aug 5.
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. |
83(1,1,1,3) |