The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands

Bioorganic & Medicinal Chemistry Letters
Robert R WilkeningSusan P Rohrer

Abstract

Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.

References

Jun 11, 1996·Proceedings of the National Academy of Sciences of the United States of America·G G KuiperJ A Gustafsson
Dec 3, 2002·Journal of Medicinal Chemistry·Brad R HenkeMillard H Lambert
Dec 14, 2002·Lancet·Vered StearnsDanielF Hayes
Apr 15, 2004·Bioorganic & Medicinal Chemistry Letters·Wu YangJohn K Dickson
May 6, 2004·Bioorganic & Medicinal Chemistry Letters·Seongkon KimMilton L Hammond
Sep 3, 2004·Bioorganic & Medicinal Chemistry Letters·Michael D ColliniChris P Miller
Oct 1, 2004·Journal of Medicinal Chemistry·Michael S MalamasHeather A Harris
Aug 16, 2005·Bioorganic & Medicinal Chemistry Letters·An T VuRichard E Mewshaw
Oct 13, 2005·Bioorganic & Medicinal Chemistry Letters·Richard ChesworthPaul DaSilva-Jardine

❮ Previous
Next ❯

Citations

Apr 4, 2014·Chemical & Pharmaceutical Bulletin·Kiminori OhtaYasuyuki Endo
Aug 28, 2014·International Journal of Environmental Research and Public Health·Hui Wen NgHuixiao Hong
Sep 30, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·Tiziano TuccinardiAdriano Martinelli
May 30, 2013·Expert Opinion on Therapeutic Patents·Ilaria PaterniFilippo Minutolo
Dec 8, 2009·Medicinal Research Reviews·Filippo MinutoloJohn A Katzenellenbogen
Jun 17, 2006·Bioorganic & Medicinal Chemistry Letters·Dann L ParkerMilton L Hammond
May 30, 2006·Bioorganic & Medicinal Chemistry Letters·R R WilkeningM L Hammond
Mar 23, 2010·Expert Opinion on Therapeutic Patents·Michael L MohlerJames T Dalton
Jul 7, 2007·Physiological Reviews·Nina HeldringJan-Ake Gustafsson
Feb 14, 2008·Journal of Medicinal Chemistry·Filippo MinutoloMarco Macchia
May 24, 2007·Journal of Pharmaceutical Sciences·Joseph V TurnerBeverley D Glass

❮ 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.

Related Papers

Bioorganic & Medicinal Chemistry Letters
Dann L ParkerMilton L Hammond
Bioorganic & Medicinal Chemistry Letters
Richard ChesworthPaul DaSilva-Jardine
Medicinal Research Reviews
Filippo MinutoloJohn A Katzenellenbogen
© 2022 Meta ULC. All rights reserved