Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands

Autor:	Dennis Heyer, Lisa A. Orband-Miller, Frank Navas, David W. Gray, Shawn P. Williams, Adwoa Akwabi-Ameyaw, Jean Shearin, Jing Fang, Subba Reddy Katamreddy, Aaron B. Miller, Jonathan E. Britton
Rok vydání:	2008
Předmět:	Selective Estrogen Receptor Modulators Stereochemistry Clinical Biochemistry Pharmaceutical Science Estrogen receptor Ether Naphthalenes Ligands Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Estrogen Receptor Modulators Drug Discovery Combinatorial Chemistry Techniques Estrogen Receptor beta Humans Structure–activity relationship Molecular Biology Alkyl Estrogen receptor beta chemistry.chemical_classification Molecular Structure Organic Chemistry Estrogen Receptor alpha Ligand (biochemistry) Receptors Estrogen chemistry Molecular Medicine Female Estrogen receptor alpha
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:5075-5077
ISSN:	0960-894X
Popis:	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:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2de6665b6284851455d32b240179f635 https://doi.org/10.1016/j.bmcl.2008.07.121 Zobrazit plný text záznamu Full Text from ScienceDirect