Results 41 to 50 of about 12,682 (158)

Novel Indoline Spiropyrans Based on Human Hormones β-Estradiol and Estrone: Synthesis, Structure, Chromogenic and Cytotoxic Properties

Molecules, 2023
The introduction of a switchable function into the structure of a bioactive compound can endow it with unique capabilities for regulating biological activity under the influence of various types of external stimuli, which makes such hybrid compounds ...
Ilya V. Ozhogin, Artem D. Pugachev, Nadezhda I. Makarova, Anna A. Belanova, Anastasia S. Kozlenko, Irina A. Rostovtseva, Peter V. Zolotukhin, Oleg P. Demidov, Islam M. El-Sewify, Gennady S. Borodkin, Anatoly V. Metelitsa, Boris S. Lukyanov   +11 more
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Design, Synthesis, and Evaluation of Novel 2-Methoxyestradiol Derivatives as Apoptotic Inducers through an Intrinsic Apoptosis Pathway

Biomolecules, 2020
In order to discover novel derivatives in the anti-tumor field, reported anti-tumor pharmacophores (uridine, uracil, and thymine) were combined with 2-methoxyestradiol, which has been characterized as having excellent biological properties in terms of ...
Li-Xin Sheng, Jiang-Yu Zhang, Li Li, Xiao Xie, Xiao-An Wen, Ke-Guang Cheng   +5 more
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Zearalenone and the Immune Response

Toxins, 2021
Zearalenone (ZEA) is an estrogenic fusariotoxin, being classified as a phytoestrogen, or as a mycoestrogen. ZEA and its metabolites are able to bind to estrogen receptors, 17β-estradiol specific receptors, leading to reproductive disorders which include ...
Cristina Valeria Bulgaru, Daniela Eliza Marin, Gina Cecilia Pistol, Ionelia Taranu   +3 more
doaj   +1 more source

Nordihydroguaiaretic Acid as a Novel Substrate and Inhibitor of Catechol O-Methyltransferase Modulates 4-Hydroxyestradiol-Induced Cyto- and Genotoxicity in MCF-7 Cells

Molecules, 2021
Nordihydroguaiaretic acid (NDGA) is a major lignan metabolite found in Larrea spp., which are widely used in South America to treat various diseases. In breast tissue, estradiol is metabolized to the catechol estrogens such as 4-hydroxyestradiol (4-OHE2),
Jin-Hee Kim, Jimin Lee, Hyesoo Jeong, Mi Seo Bang, Jin-Hyun Jeong, Minsun Chang   +5 more
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Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents [PDF]

Letters in Drug Design & Discovery, 2010
3-N-alkyloxyestradiol derivatives were synthesized, characterized and tested for activity in MCF-7 human breast cancer cells. Among the compounds, the diisopropyl and piperidinyl derivatives were found to be more active than 4-hydroxytamoxifen (HO-Tam), the active metabolite of tamoxifen based upon IC(50) values.
John S, Cooperwood, Jesse, Edwards, Musiliyu, Musa, Devora, Simmons, Abdul D, Mian, Kwon-Kyun, Park, Zhongliang, Wan   +6 more
openaire   +2 more sources

An amphioxus orthologue of the estrogen receptor that does not bind estradiol: Insights into estrogen receptor evolution

BMC Evolutionary Biology, 2008
Background The origin of nuclear receptors (NRs) and the question whether the ancestral NR was a liganded or an unliganded transcription factor has been recently debated.
Laudet Vincent, Escriva Hector, Pongratz Ingemar, Bertrand Stephanie, Pettersson Katarina, Schubert Michael, Paris Mathilde   +6 more
doaj   +1 more source

Comparative Solution Equilibrium Studies on Anticancer Estradiol-Based Conjugates and Their Copper Complexes

Inorganics
Steroids are often considered valuable molecular tools for the development of anticancer agents with improved pharmacological properties. Conjugation of metal chelating moieties with a lipophilic sterane backbone is a viable option to obtain novel ...
Éva A. Enyedy, Anett Giricz, Tatsiana V. Petrasheuskaya, János P. Mészáros, Nóra V. May, Gabriella Spengler, Ferenc Kovács, Barnabás Molnár, Éva Frank   +8 more
doaj   +1 more source

Synthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various 15β-oxa-linked substituents and hydroxy, methoxy, benzyloxy, and sulfamate groups in position C3 as ...
Bianka Edina Herman, Anita Kiss, János Wölfling, Erzsébet Mernyák, Mihály Szécsi, Gyula Schneider   +5 more
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Coincidence of Persistent Müllerian duct syndrome and testicular tumors in dogs

BMC Veterinary Research, 2017
Background Persistent Müllerian duct syndrome (PMDS), a rare form of male pseudohermaphroditism in dogs, is an abnormal sexual phenotype in males that is characterized by the existence of a hypoplastic oviduct, uterus, and cranial part of the vagina ...
Eun Jung Park, Seok-Hee Lee, Young-Kwang Jo, Sang-Eun Hahn, Do-Min Go, Su-Hyung Lee, Byeong-Chun Lee, Goo Jang   +7 more
doaj   +1 more source

Mesyl chloride-mediated synthesis and in vitro anticancer evaluation of 2-carboxamide derivatives of estrone and estradiol

Results in Chemistry
The 2-carboxamide derivatives of estrone (E1) and estradiol (E2) offer untapped anticancer potential, mimicking active 2-methoxyestradiol (2ME2). We synthesized a 12-member library via a mesyl chloride (MsCl)-mediated protocol that overcame steric ...
András Novák, Barnabás Molnár, Ildikó Huliák, Hédi Árva, Eszter Nagy, Zoltán Kele, Mónika Kiricsi, Éva Frank   +7 more
doaj   +1 more source