179 articles for thisTarget
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Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.
Astrazeneca
A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptorsa andß.
Purdue University
Synthesis, antiproliferative and pro-apoptotic activity of 2-phenylindoles.
Trinity College
Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
German University In Cairo
Synthesis, estrogenic activity, and anti-osteoporosis effects in ovariectomized rats of resveratrol oligomer derivatives.
Fudan University
Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University)
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
TBA
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Seragon Pharmaceuticals
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.
Purdue University
2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists.
TBA
Highly selective salicylketoxime-based estrogen receptorß agonists display antiproliferative activities in a glioma model.
Universit£
ß-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.
Trinity College
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.
Astrazeneca
Identification of the first potent, selective and bioavailable PPARa antagonist.
Inception Sciences
Triaryl-substituted Schiff bases are high-affinity subtype-selective ligands for the estrogen receptor.
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University)
Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character.
The University of Tokyo
Thiophene-core estrogen receptor ligands having superagonist activity.
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University)
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer.
Trinity College
Synthesis and biochemical characterization of a series of 17a-perfluoroalkylated estradiols as selective ligands for estrogen receptora.
Charles University In Prague
QSAR of estrogen receptor modulators: exploring selectivity requirements for ER(alpha) versus ER(beta) binding of tetrahydroisoquinoline derivatives using E-state and physicochemical parameters.
University of Calcutta
Influence of chlorine or fluorine substitution on the estrogenic properties of 1-alkyl-2,3,5-tris(4-hydroxyphenyl)-1H-pyrroles.
Freie Universit£T Berlin
Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins.
Rwth Aachen University
Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening.
East China University of Science and Technology
Identification and structure-activity relationships of a novel series of estrogen receptor ligands based on 7-thiabicyclo[2.2.1]hept-2-ene-7-oxide.
Wuhan University
Recent advances in the synthesis of raloxifene: a selective estrogen receptor modulator.
Torrey Pines Institute For Molecular Studies
Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents.
Johnson & Johnson Pharmaceutical Research and Development
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
Chinese Academy of Sciences
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening.
East China University of Science and Technology
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.
Wyeth Research
Synthesis and biological evaluation of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core.
Fin-00014 University of Helsinki
"Virtual fragment linking": an approach to identify potent binders from low affinity fragment hits.
Novartis Institutes For Biomedical Research
Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta.
Universita Di Pisa
Design, synthesis, and estrogenic activity of a novel estrogen receptor modulator--a hybrid structure of 17beta-estradiol and vitamin E in hippocampal neurons.
University of Southern California
Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.
University of Southern California
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
Abbott Laboratories
De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.
Signalgene
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
Pfizer
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase.
Novartis Forschungsinstitut
Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity.
Kyoto Pharmaceutical University
Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.
Wyeth-Ayerst Research
Diarylpropionitrile (DPN) enantiomers: synthesis and evaluation of estrogen receptorß-selective ligands.
University of Illinois
Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes.
Universit£
Design and evaluation of fragment-like estrogen receptor tetrahydroisoquinoline ligands from a scaffold-detection approach.
Technische Universiteit Eindhoven
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements.
University of Delaware
Virtual and biomolecular screening converge on a selective agonist for GPR30.
University of New Mexico Health Sciences Center
Bioactivity-guided mapping and navigation of chemical space.
Institut FüR Molekulare Physiologie
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
New estrogenic compounds isolated from Broussonetia kazinoki.
Sookmyung Women'S University
Synthesis and evaluation of 17alpha-arylestradiols as ligands for estrogen receptor alpha and beta.
Academy of Sciences of The Czech Republic
LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.
The University of Tokyo
Isoflavonoids from Erythrina poeppigiana: evaluation of their binding affinity for the estrogen receptor.
University of Athens
Identification and structure-activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms.
Johnson & Johnson Pharmaceutical Research & Development
Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta.
University of Illinois
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
Glaxosmithkline
Phenethyl pyridines with non-polar internal substituents as selective ligands for estrogen receptor beta.
University of Illinois
Steroidal bivalent ligands for the estrogen receptor: design, synthesis, characterization and binding affinities.
University of Illinois At Urbana-Champaign
Synthesis and evaluation of aryl-substituted diarylpropionitriles, selective ligands for estrogen receptor beta, as positron-emission tomographic imaging agents.
Institute of Radiological and Medical Sciences
Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor beta.
University of Pittsburgh
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.
Pfizer
Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta.
Universita Di Pisa
Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators.
Trinity College
Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding.
University of Illinois At Urbana-Champaign
Promising core structure for nuclear receptor ligands: design and synthesis of novel estrogen receptor ligands based on diphenylamine skeleton.
Tohoku Pharmaceutical University
Classification of estrogen receptor-beta ligands on the basis of their binding affinities using support vector machine and linear discriminant analysis.
Yantai University
Pochonins A-F, new antiviral and antiparasitic resorcylic acid lactones from Pochonia chlamydosporia var. catenulata.
Bayer Healthcare
Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis.
Université
Target specific virtual screening: optimization of an estrogen receptor screening platform.
Trinity College
Estrogen receptor dependent inhibitors of NF-kappaB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives: pathway selective inhibitors of NF-kappaB, a potential treatment for rheumatoid arthritis.
Wyeth Research
Aza analogues of equol: novel ligands for estrogen receptor beta.
Chinese Academy of Sciences
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.
Eli Lilly
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.
Merck Research Laboratories
ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives.
Wyeth Research
Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones.
Wyeth Research
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.
Irbm (Merck Research Laboratories Rome)
Synthesis of anthranylaldoxime derivatives as estrogen receptor ligands and computational prediction of binding modes.
Università
Tetrahydrofluorenones with conformationally restricted side chains as selective estrogen receptor beta ligands.
Merck Research Laboratories
Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.
Merck Research Laboratories
Estrogen receptor beta-subtype selective tetrahydrofluorenones: use of a fused pyrazole as a phenol bioisostere.
Merck Research Laboratories
Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
Johnson & Johnson Pharmaceutical Research & Development
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.
Merck Research Laboratories
6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists.
Merck Research Laboratories
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Pfizer
Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
Merck Research Laboratories
Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands.
University of California
ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives.
Wyeth Research
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.
Merck Research Laboratories
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.
Wyeth Research
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.
Merck Research Laboratories
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.
Chinese Academy of Sciences
Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.
Wyeth Research
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs.
Merck Research Laboratories
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.
Chinese Academy of Sciences
Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold.
Ligand Pharmaceuticals
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
Merck Research Laboratories
Investigations on the effects of basic side chains on the hormonal profile of (4R,5S)/(4S,5R)-4,5-bis(4-hydroxyphenyl)-2-imidazolines.
Free University of Berlin
Synthesis and activity of substituted 4-(indazol-3-yl)phenols as pathway-selective estrogen receptor ligands useful in the treatment of rheumatoid arthritis.
Wyeth Research
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.
Merck Research Laboratories
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
Wyeth Research
Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.
Merck Research Laboratories
Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.
Merck Research Laboratories
Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.
Merck Research Laboratories
Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains.
Merck Research Laboratories
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
Merck Research Laboratories
Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.
Merck Research Laboratories
Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.
Merck Research Laboratories
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.
Merck Research Laboratories
Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree!
Merck Research Laboratories
B-ring unsaturated estrogens: biological evaluation of 17alpha-Dihydroequilein and novel B-Nor-6-thiaequilenins as tissue selective estrogens.
Eli Lilly
Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process.
Università
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).
Merck Research Laboratories
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.
Glaxosmithkline
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
University of Illinois
Furans with basic side chains: synthesis and biological evaluation of a novel series of antagonists with selectivity for the estrogen receptor alpha.
University of Illinois
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.
Glaxo Wellcome Research and Development
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
Wyeth-Ayerst Research
Structural features underlying raloxifene's biophysical interaction with bone matrix.
Lilly Research Laboratories
Probing the human estrogen receptor-? binding requirements for phenolic mono- and di-hydroxyl compounds: a combined synthesis, binding and docking study.
Marquette University
Discovery of natural estrogen receptor modulators with structure-based virtual screening.
East China University of Science and Technology
Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.
Glaxosmithkline Research & Development
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs).
Marquette University
Estrogen Receptor (ER) Subtype Selectivity Identifies 8-Prenylapigenin as an ER? Agonist from Glycyrrhiza inflata and Highlights the Importance of Chemical and Biological Authentication.
TBA
Recent advances in peptidomimetics antagonists targeting estrogen receptor ?-coactivator interaction in cancer therapy.
Peking University Shenzhen Graduate School
Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ER? and ER? Activity.
Trinity College
Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer.
Wuhan University
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Astrazeneca
Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17?-Hydroxysteroid Dehydrogenase Type 2.
University of Basel
Dehydrodiconiferyl Alcohol Inhibits Osteoclast Differentiation and Ovariectomy-Induced Bone Loss through Acting as an Estrogen Receptor Agonist.
Seoul National University
Indazole-based ligands for estrogen-related receptor ? as potential anti-diabetic agents.
Janssen Research and Development
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
Kyushu University
Dual functional small molecule fluorescent probes for image-guided estrogen receptor-specific targeting coupled potent antiproliferative potency for breast cancer therapy.
Wuhan University School of Pharmaceutical Sciences
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Astrazeneca
Structural Basis of Inhibition of ER?-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides.
Shenzhen Graduate School of Peking University
Design, synthesis, molecular docking, anti-Proteus mirabilis and urease inhibition of new fluoroquinolone carboxylic acid derivatives.
Minia University
Systems-based design of bi-ligand inhibitors of oxidoreductases: filling the chemical proteomic toolbox.
Triad Therapeutics
Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.
Cyclacel
Inhibitor specificity via protein dynamics: insights from the design of antibacterial agents targeted against thymidylate synthase.
UniversitÀ
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: part 2.
Schering-Plough Research Institute
Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids).
University of Auckland
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.
Boehringer Ingelheim Pharmaceuticals