Results 11 to 20 of about 744,343 (249)

Chemical Synthesis and Biological Evaluation of 3-Substituted Estrone/Estradiol Derivatives as 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors Acting via a Reverse Orientation of the Natural Substrate Estrone [PDF]

Molecules, 2023
Estradiol (E2) plays an important role in the progression of diseases such as breast cancer and endometriosis. Inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), the enzyme that catalyzes the last step in the biosynthesis of the estrogenic
Adrien Djiemeny Ngueta, Jenny Roy, René Maltais, Donald Poirier   +3 more
doaj   +2 more sources

Preparation of 16β-Estradiol Derivative Libraries as Bisubstrate Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 Using the Multidetachable Sulfamate Linker

Molecules, 2010
Combinatorial chemistry is a powerful tool used to rapidly generate a large number of potentially biologically active compounds. In our goal to develop bisubstrate inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) that interact with both ...
Donald Poirier, Florian Delagoutte, Marie Bérubé   +2 more
doaj   +2 more sources

Correction to: Novel sulphamoylated 2-methoxy estradiol derivatives inhibit breast cancer migration by disrupting microtubule turnover and organization [PDF]

Cancer Cell International, 2020
An amendment to this paper has been published and can be accessed via the original article.
Rustelle Janse van Vuuren, Mandie Botes, Tamarin Jurgens, Anna Margaretha Joubert, Iman van den Bout   +4 more
doaj   +2 more sources

Novel sulphamoylated 2-methoxy estradiol derivatives inhibit breast cancer migration by disrupting microtubule turnover and organization [PDF]

Cancer Cell International, 2019
Background The estrogen metabolite 2-methoxyestradiol (2ME2) and a number of synthesised derivatives have been shown to bind to microtubules thereby arresting cancer cells in mitosis which leads to apoptosis.
Rustelle Janse van Vuuren, Mandie Botes, Tamarin Jurgens, Anna Margaretha Joubert, Iman van den Bout   +4 more
doaj   +2 more sources

Retention behaviour of some estradiol derivatives on alumina in normal phase chromatography [PDF]

Journal of the Serbian Chemical Society, 2003
The retention constants of variously substituted estradiol derivatives were measured as a function of the composition of various binary mobile phases in order to study the relationship between chemical structure and retention behaviour in TLC on alumina.
MARIJANA M. ACANSKI
doaj   +1 more source

Menopause hormone therapy in women with cardiovascular risk factors or established ischemic heart disease: A joint FIGO and WHF position paper [PDF]

International Journal of Gynecology &Obstetrics, EarlyView.
Integrated approach to menopausal hormone therapy in women with cardiovascular risk factors or established ischemic heart disease, from early treatment initiation and risk stratification to individualized therapy, multidisciplinary follow‐up, and health‐system recommendations.
Chiara Benedetto, Martha Gulati, Suvarna S. Khadilkar, Angela H. E. M. Maas, Federica Frezet, Gláucia Maria Moraes de Oliveira, Andrea R. Genazzani, Hema Divakar, Athena Poppas, on behalf of the World Heart Federation (WHF) and the International Federation of Gynecology and Obstetrics (FIGO)   +9 more
wiley   +2 more sources

Novel SOAT inhibitors block DHEAS transport and suppress proliferation in MCF-7 breast cancer cells [PDF]

Scientific Reports
Intracrine estrogen formation from adrenal precursors such as dehydroepiandrosterone sulfate (DHEAS) plays a critical role in sustaining estrogen receptor (ER)-positive breast cancer cell proliferation, particularly in postmenopausal women.
Emre Karakus, Silke Leiting, Michael Daude, Wibke E. Diederich, Joachim Geyer   +4 more
doaj   +2 more sources

Estradiol regulation of nucleotidases in female reproductive tract epithelial cells and fibroblasts. [PDF]

PLoS ONE, 2013
The use of topical and oral adenosine derivatives in HIV prevention that need to be maintained in tissues and cells at effective levels to prevent transmission prompted us to ask whether estradiol could influence the regulation of catabolic nucleotidase ...
Zheng Shen, John V Fahey, Jack E Bodwell, Marta Rodriguez-Garcia, Richard M Rossoll, Sarah G Crist, Mickey V Patel, Charles R Wira   +7 more
doaj   +1 more source

C-Ring Oxidized Estrone Acetate Derivatives: Assessment of Antiproliferative Activities and Docking Studies

Applied Sciences, 2022
C-Ring oxidized estrone acetate derivatives as antiproliferative agents were prepared and tested against five cancer cell lines by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay.
Catarina Canário, Mariana Matias, Vanessa Brito, Patrícia Pires, Adriana O. Santos, Amílcar Falcão, Samuel Silvestre, Gilberto Alves   +7 more
doaj   +1 more source

Dose-response effects of estrogenic mycotoxins (zearalenone, alpha- and beta-zearalenol) on motility, hyperactivation and the acrosome reaction of stallion sperm

Reproductive Biology and Endocrinology, 2011
Background The aim of this study was to investigate the in vitro effects of the Fusarium fungus-derived mycotoxin, zearalenone and its derivatives alpha-zearalenol and beta-zearalenol on motility parameters and the acrosome reaction of stallion sperm ...
Colenbrander Ben, Pizzi Flavia, Sostaric Edita, Gadella Bart M, Stout Tom AE, Filannino Angela, Dell'Aquila Maria, Minervini Fiorenza   +7 more
doaj   +1 more source