Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands.
Article Details
- CitationCopy to clipboard
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. doi: 10.1016/j.bmcl.2008.07.121. Epub 2008 Aug 5.
- PubMed ID
- 18722117 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Estradiol Estrogen receptor alpha Ki (nM) 2 N/A N/A Details Estradiol Estrogen receptor beta Ki (nM) 2 N/A N/A Details Raloxifene Estrogen receptor alpha Ki (nM) 2 N/A N/A Details Raloxifene Estrogen receptor beta Ki (nM) 23 N/A N/A Details