PMID: 11906280Mar 22, 2002Paper

Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes

Journal of Medicinal Chemistry
Ulrich SchopferPhilipp Floersheim

Abstract

In an effort to identify selective ligands for the estrogen receptor subtype ERbeta, a series of aryl benzthiophenes was synthesized. In a radioligand binding assay and reporter gene assays in HeLa and SH-SY5Y cells, compounds were characterized as ERbeta-selective agonists. By targeting ERbeta in the brain, these compounds could lead to drugs able to separate the beneficial effects of estrogens on mood, learning, and memory from side effects such as the stimulation of endometrial and breast cancer.

References

Jun 11, 1996·Proceedings of the National Academy of Sciences of the United States of America·G G KuiperJ A Gustafsson
Oct 24, 1997·Nature·A M BrzozowskiM Carlquist
Dec 5, 1997·The Journal of Comparative Neurology·P J ShughrueI Merchenthaler
Jun 16, 1999·Endocrine Reviews·J F Couse, K S Korach
Mar 7, 2000·Current Medicinal Chemistry·K DecheringS Mosselman
Apr 12, 2000·Proceedings of the National Academy of Sciences of the United States of America·R StrickJ D Rowley
Jul 25, 2000·Toxicology Letters·G Boos, H Stopper

❮ Previous
Next ❯

Citations

Feb 26, 2004·Bioorganic & Medicinal Chemistry Letters·Timothy A BlizzardMilton L Hammond
Apr 15, 2004·Bioorganic & Medicinal Chemistry Letters·Wu YangJohn K Dickson
May 7, 2005·Bioorganic & Medicinal Chemistry Letters·Robert E McDevittHeather A Harris
May 7, 2004·Journal of Pharmaceutical and Biomedical Analysis·Theo de BoerKees Ensing
Jun 26, 2003·Bioorganic & Medicinal Chemistry Letters·Chris P MillerHeather A Harris
Jul 25, 2003·Bioorganic & Medicinal Chemistry·Richard J EdsallRichard E Mewshaw
Jul 3, 2009·Journal of Combinatorial Chemistry·Chul-Hee ChoRichard C Larock
Jan 9, 2010·Journal of Combinatorial Chemistry·Chul-Hee ChoRichard C Larock
Mar 17, 2009·European Journal of Medicinal Chemistry·Michael WaibelJohn A Katzenellenbogen
Dec 8, 2009·Medicinal Research Reviews·Filippo MinutoloJohn A Katzenellenbogen
May 21, 2016·Cell Chemical Biology·Ian CookThomas S Leyh
Dec 8, 2004·Bioorganic & Medicinal Chemistry Letters·Timothy A BlizzardMilton L Hammond
Sep 3, 2004·Bioorganic & Medicinal Chemistry Letters·Michael D ColliniChris P Miller
Jun 17, 2006·Bioorganic & Medicinal Chemistry Letters·Dann L ParkerMilton L Hammond
Apr 25, 2006·Bioorganic & Medicinal Chemistry Letters·R R WilkeningS P Rohrer
Nov 29, 2005·Bioorganic & Medicinal Chemistry Letters·Timothy A BlizzardMilton L Hammond
May 30, 2006·Bioorganic & Medicinal Chemistry Letters·R R WilkeningM L Hammond
Jul 1, 2004·Bioorganic & Medicinal Chemistry Letters·Timothy A BlizzardMilton L Hammond
Mar 23, 2010·Expert Opinion on Therapeutic Patents·Michael L MohlerJames T Dalton
Sep 23, 2003·Endocrinology·Heather A HarrisJames C Keith
Jan 22, 2013·Chemistry : a European Journal·Cheng-Han LinMing-Jung Wu
Dec 3, 2002·Journal of Medicinal Chemistry·Brad R HenkeMillard H Lambert
Mar 6, 2013·The Journal of Organic Chemistry·Caterina ViglianisiStefano Menichetti
Oct 9, 2012·Organic Letters·Durga Prasad HariBurkhard König
Aug 5, 2011·The Journal of Organic Chemistry·Lei-Lei SunXing-Guo Zhang
Mar 28, 2006·Journal of Chemical Information and Modeling·Stuart Firth-ClarkWilliam Harris
Nov 19, 2004·Journal of the American Chemical Society·Eric S ManasJuan C Alvarez
Oct 1, 2004·Journal of Medicinal Chemistry·Michael S MalamasHeather A Harris
Feb 18, 2005·Journal of Medicinal Chemistry·Meri De AngelisJohn A Katzenellenbogen

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.