388 articles for thisTarget
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Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.
The Scripps Research Institute
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERa+ Breast Cancer.
Novartis Institutes For Biomedical Research
Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.
University of Illinois College of Pharmacy
An in-tether sulfoxide chiral center influences the biophysical properties of the N-capped peptides.
Peking University Shenzhen Graduate School
Rational Design of a Boron-Modified Triphenylethylene (GLL398) as an Oral Selective Estrogen Receptor Downregulator.
Xavier University of Louisiana
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.
Astrazeneca
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.
University of Michigan
A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptorsa andß.
Purdue University
Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists.
Daegu-Gyeongbuk Medical Innovation Foundation
Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERa and VEGFR-2 as anti-breast cancer agents.
China Pharmaceutical University
Synthesis, antiproliferative and pro-apoptotic activity of 2-phenylindoles.
Trinity College
Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator.
National Institute of Health Sciences
Identification of novel estrogen receptor (ER) agonists that have additional and complementary anti-cancer activities via ER-independent mechanism.
Kyung Hee University
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists.
Vitae Pharmaceuticals
Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
German University In Cairo
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
Astrazeneca
Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer.
University of Illinois At Chicago
Peptide-based inhibitors of protein-protein interactions.
Wroclaw University of Technology
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
Astrazeneca
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.
University of Bath
Structural development of stabilized helical peptides as inhibitors of estrogen receptor (ER)-mediated transcription.
National Institute of Health Sciences
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 evaluation of tamoxifen derivatives with a long alkyl side chain as selective estrogen receptor down-regulators.
National Institute of Health Sciences
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
Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.
Astrazeneca
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.
University of Pisa
3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.
Novartis Institutes For Biomedical Research
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Bristol-Myers Squibb
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
Novel estrogen receptor (ER) modulators containing various hydrophobic bent-core structures.
Tohoku Pharmaceutical University
Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells.
Georgetown University
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.
Astrazeneca
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.
Pfizer
Synthesis and antiestrogenic activity of [3,4-dihydro-2-(4-methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]-phenyl]methanone, methanesulfonic acid salt.
TBA
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Merck Research Laboratories
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
2-Morpholinoisoflav-3-enes as flexible intermediates in the synthesis of phenoxodiol, isophenoxodiol, equol and analogues: vasorelaxant properties, estrogen receptor binding and Rho/RhoA kinase pathway inhibition.
University of Melbourne
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
Effects of C2-alkylation, N-alkylation, and N,N'-dialkylation on the stability and estrogen receptor interaction of (4R,5S)/(4S,5R)-4,5-bis(4-hydroxyphenyl)-2-imidazolines.
Free University of Berlin
(4R,5S)/(4S,5R)-4,5-Bis(4-hydroxyphenyl)-2-imidazolines: ligands for the estrogen receptor with a novel binding mode.
Free University of Berlin
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
Synthesis and evaluation of 11ß-(4-substituted phenyl) estradiol analogs: transition from estrogen receptor agonists to antagonists.
Northeastern University
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
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.
Bristol-Myers Squibb
Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation.
Freie Universit£T Berlin
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.
Pfizer
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
Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone.
Institute of Experimental Genetics
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
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.
Bristol-Myers Squibb
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
Wyeth Research
Estrogenic and anticarcinogenic properties of kurarinone, a lavandulyl flavanone from the roots of Sophora flavescens.
Ghent University
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Wyeth 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
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Abbott Laboratories
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
Investigation of the diastereomerism of dihydrobenzoxathiin SERMs for ER alpha by molecular modeling.
Zhejiang University
Recent progress in synthesis and bioactivity studies of indolizines.
University of Botswana
Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.
Kaken Pharmaceutical
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791
Bristol-Myers Squibb
DNA site-specific N3-adenine methylation targeted to estrogen receptor-positive cells.
University of North Carolina At Wilmington
Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes.
University of Pisa
Estrogenic activity of chemical constituents from Tephrosia candida.
National Research Centre
Design and evaluation of fragment-like estrogen receptor tetrahydroisoquinoline ligands from a scaffold-detection approach.
Technische Universiteit Eindhoven
Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor.
Chinese Academy of Sciences
Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs.
Institute of Theoretical Studies Ggmbh
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
Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells.
Xavier University of Louisiana
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
Instituto PolitéCnico Nacional 2508
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
Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery.
Pfizer
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.
Pfizer
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
Click synthesis of estradiol-cyclodextrin conjugates as cell compartment selective estrogens.
University of Illinois At Chicago
Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.
Sumitomo Chemical
Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta.
University of Illinois
Phenethyl pyridines with non-polar internal substituents as selective ligands for estrogen receptor beta.
University of Illinois
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Merck Research Laboratories
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
Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity.
University of Illinois
Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor.
University of Illinois At Urbana-Champaign
Cobalt-alkyne complexes with imidazoline ligands as estrogenic carriers: synthesis and pharmacological investigations.
Freie Universitat Berlin
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
Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis.
Université
Three new arylobenzofurans from Onobrychis ebenoides and evaluation of their binding affinity for the estrogen receptor.
University of Athens
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Eli Lilly
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
The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents.
University of South China
Aza analogues of equol: novel ligands for estrogen receptor beta.
Chinese Academy of Sciences
Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators.
University of Illinois
Selective Estrogen receptor degraders (SERDs) for the treatment of breast cancer: An overview.
Central University of Punjab
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety.
Eli Lilly
Identification of Novel Dual-Target Estrogen Receptor α Degraders with Tubulin Inhibitory Activity for the Treatment of Endocrine-Resistant Breast Cancer.
Zhongnan Hospital of Wuhan University
Synthesis, characterization, and estrogen receptor binding affinity of flavone-, indole-, and furan-estradiol conjugates.
Université
Targeting the Estrogen Receptor for the Treatment of Breast Cancer: Recent Advances and Challenges.
University of Michigan
Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer
Zhongnan Hospital of Wuhan University
Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.
Guangdong Pharmaceutical University
Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents.
University of Sharjah
Discovery of a Novel Bifunctional Steroid Analog, YXG-158, as an Androgen Receptor Degrader and CYP17A1 Inhibitor for the Treatment of Enzalutamide-Resistant Prostate Cancer.
Shanghai Institute of Materia Medica
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.
Merck Research Laboratories
Synthesis, structure, and estrogenic activity of 4-amino-3-(2-methylbenzyl)coumarins on human breast carcinoma cells.
Equipe De Chimie ThéRapeutique
Structure-guided identification of novel dual-targeting estrogen receptor α degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast cancer.
Zhongnan Hospital of Wuhan University
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
Dammarane-type leads panaxadiol and protopanaxadiol for drug discovery: Biological activity and structural modification.
Shenyang Pharmaceutical University
Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer.
Nanjing University of Chinese Medicine
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
Recent advances in combretastatin A-4 codrugs for cancer therapy.
Xinxiang Medical University
Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.
Merck Research Laboratories
Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer.
Wuhan University
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
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis.
Southern Medical University Biomedical Research Center
6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists.
Merck Research Laboratories
Substituted 4-hydroxyphenyl sulfonamides as pathway-selective estrogen receptor ligands.
Wyeth Research
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
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.
Wyeth Research
A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3-
University of North Carolina
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
Rational design, synthesis, antiproliferative activity against MCF-7, MDA-MB-231 cells, estrogen receptors binding affinity, and computational study of indenopyrimidine-2,5-dione analogs for the treatment of breast cancer.
Comsats University Islamabad
Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.
Wyeth Research
Human estrogen receptor α antagonists, part 2: Synthesis driven by rational design, in vitro antiproliferative, and in vivo anticancer evaluation of innovative coumarin-related antiestrogens as breast cancer suppressants.
University of Kragujevac
An overview on Estrogen receptors signaling and its ligands in breast cancer.
Zhejiang University
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs.
Merck Research Laboratories
Cascade synthetic strategies opening access to medicinal-relevant aliphatic 3- and 4-membered N-heterocyclic scaffolds.
Adam Mickiewicz University
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
Discovery of two novel (4-hydroxyphenyl) substituted polycyclic carbocycles as potent and selective estrogen receptor beta agonists.
Marquette University
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
Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.
Central University of Punjab
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
Searching for an ideal SERM: Mining tamoxifen structure-activity relationships.
University of Texas At Austin
Heterodimeric GW7604 Derivatives: Modification of the Pharmacological Profile by Additional Interactions at the Coactivator Binding Site.
University of Innsbruck
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
Wyeth Research
Activable Targeted Protein Degradation Platform Based on Light-triggered Singlet Oxygen.
Wuhan University of Science and Technology
Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer.
Alma Mater Studiorum-University of Bologna
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
Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer.
China Pharmaceutical University
Dynamics-Based Discovery of Novel, Potent Benzoic Acid Derivatives as Orally Bioavailable Selective Estrogen Receptor Degraders for ERα+ Breast Cancer.
Nanjing University of Chinese Medicine
Mechanistic Investigation of Site-specific DNA Methylating Agents Targeting Breast Cancer Cells.
University of North Carolina Wilmington
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
Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening.
X-Chem
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Genentech
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Discovery of chiral N-2'-aryletheryl-1'-alkoxy-ethyl substituted arylisoquinolones with anti-inflammatory activity from the nucleophilic addition reactions of the thiophenols and oxazolinium.
Chinese Academy of Sciences
Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
Wuhan University
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
Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.
Genentech
Synthesis and estrogen receptor binding affinities of 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-ones containing a basic side chain.
The Ohio State University
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents.
The Feinberg School of Medicine of Northwestern University
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.
Astrazeneca
Synthesis and evaluation of 17α-triazolyl and 9α-cyano derivatives of estradiol.
Marquette University
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).
Merck Research Laboratories
Machine Learning on DNA-Encoded Libraries: A New Paradigm for Hit Finding.
Google Research Applied Science, Mountain View, California 94043, United States.
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.
Glaxosmithkline
Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes.
Free University of Berlin
Synthesis and structure-activity relationships of 1-benzylindane derivatives as selective agonists for estrogen receptor beta.
Kissei Pharmaceutical
Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.
Purdue University
Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators.
Bayer Research Center
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Endotherm
An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
Daegu-Gyeongbuk Medical Innovation Foundation
Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD).
Luoxin Pharmaceutical (Shanghai) Co.
Discovery of bazedoxifene analogues targeting glycoprotein 130.
China Pharmaceutical University
Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.
University of Innsbruck
Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
Daegu-Gyeongbuk Medical Innovation Foundation
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Tes Pharma
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Astrazeneca
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
University of Illinois
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.
University of Illinois At Chicago
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
Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening.
Trinity College
Bisphenol AF: Halogen bonding effect is a major driving force for the dual ERα-agonist and ERβ-antagonist activities.
Kyushu University
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
Wyeth-Ayerst Research
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
Genentech
Phosphine boranes as less hydrophobic building blocks than alkanes and silanes: Structure-property relationship and estrogen-receptor-modulating potency of 4-phosphinophenol derivatives.
The University of Tokyo
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
University of Naples "Federico Ii
Antiausterity Activity of Secondary Metabolites from the Roots of
University of Innsbruck
Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD).
Xavier University of Louisiana
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Genentech
Discovery of Potent, Selective, and Orally Bioavailable Estrogen-Related Receptor-γ Inverse Agonists To Restore the Sodium Iodide Symporter Function in Anaplastic Thyroid Cancer.
Daegu-Gyeongbuk Medical Innovation Foundation
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute of The Novartis Research Foundation (Gnf)
Structure-based drug design, synthesis, In vitro, and In vivo biological evaluation of indole-based biomimetic analogs targeting estrogen receptor-α inhibition.
The British University In Egypt
Estrogen signaling: An emanating therapeutic target for breast cancer treatment.
Indian Institute of Technology (Bhu)
Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.
University of Georgia
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.
The University of Tokyo
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.
Genentech
Selective Estrogen Receptor Degraders for the Potential Treatment of Cancer.
Usona Institute
A-C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions.
Concordia University Wisconsin
Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.
Astrazeneca
Boron in drug design: Recent advances in the development of new therapeutic agents.
S£O Paulo State University
Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index.
Helmholtz-Zentrum Dresden-Rossendorf
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
University of Illinois At Chicago
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.
Sun Yat-Sen University
Exploring the PROTAC degron candidates: OBHSA with different side chains as novel selective estrogen receptor degraders (SERDs).
Wuhan University
Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.
Seragon Pharmaceuticals
Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft.
Seragon Pharmaceuticals
Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
China Pharmaceutical University
Myrmenaphthol A, Isolated from a Hawaiian Sponge of the Genus
University of Hawaii At Manoa
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.
Astrazeneca
PROTAC-Mediated Degradation of Estrogen Receptor in the Treatment of Cancer.
Usona Institute
Symmetric 4,4'-(piperidin-4-ylidenemethylene)bisphenol derivatives as novel tunable estrogen receptor (ER) modulators.
Tohoku Pharmaceutical University
Structural features underlying raloxifene's biophysical interaction with bone matrix.
Lilly Research Laboratories
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
Mcgill University
4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors.
Northeastern University
Probing the human estrogen receptor-α binding requirements for phenolic mono- and di-hydroxyl compounds: a combined synthesis, binding and docking study.
Marquette University
3D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors.
University of Siena
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
Georgia Institute of Technology
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-β agonists (SERBAs).
Marquette University
Estrogen Receptor (ER) Subtype Selectivity Identifies 8-Prenylapigenin as an ERβ Agonist from Glycyrrhiza inflata and Highlights the Importance of Chemical and Biological Authentication.
TBA
Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives.
American University of Ras Al Khaimah
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.
Mcgill University
Recent advances in peptidomimetics antagonists targeting estrogen receptor α-coactivator interaction in cancer therapy.
Peking University Shenzhen Graduate School
Success stories of natural product-based hybrid molecules for multi-factorial diseases.
Punjabi University
Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.
China Pharmaceutical University
Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton.
Nagasaki University
Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ERα and ERβ 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
DESIGNER Extracts as Tools to Balance Estrogenic and Chemopreventive Activities of Botanicals for Women's Health.
Hallertauer Hopfenveredelung
Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators.
Central University of Punjab
Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17β-Hydroxysteroid Dehydrogenase Type 2.
University of Basel
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.
TBA
Dehydrodiconiferyl Alcohol Inhibits Osteoclast Differentiation and Ovariectomy-Induced Bone Loss through Acting as an Estrogen Receptor Agonist.
Seoul National University
Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-α).
Central University of Punjab
Disconnecting the Estrogen Receptor Binding Properties and Antimicrobial Properties of Parabens through 3,5-Substitution.
Longwood University
Selective Estrogen Receptor Degraders (SERDs): A Promising Treatment to Overcome Resistance to Endocrine Therapy in ERα-Positive Breast Cancer.
Therachem Research Medilab (India)
Novel SERMs based on 3-aryl-4-aryloxy-2H-chromen-2-one skeleton - A possible way to dual ERα/VEGFR-2 ligands for treatment of breast cancer.
China Pharmaceutical University
Indazole-based ligands for estrogen-related receptor α 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
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Pfizer
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
Novartis Institutes For Biomedical Research
Structural Basis of Inhibition of ERα-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides.
Shenzhen Graduate School of Peking University
Efficient synthesis of a multi-substituted diphenylmethane skeleton as a steroid mimetic.
National Institute of Health Sciences
TRICYCLIC COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Shanghaitech University
T-TYPE CALCIUM CHANNEL ANTAGONISTS AND USES THEREOF
The Leland Stanford Junior University
Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of sodium channel activity
Praxis Precision Medicines
Substituted pyridines as inhibitors of DNMT1
Glaxosmithkline Intellectual Property Development
Intermediate compound of novel tetrahydronaphthyl urea derivative
Mochida Pharmaceutical
Method for preparing pyrrolo[3,2-D]pyrimidine compound, and intermediates thereof
Chia Tai Tianqing Pharmaceutical Group
Quinolone derivatives as fibroblast growth factor receptor inhibitors
Principia Biopharma
1-cyclohexyl-2-phenylaminobenzimidazoles as mIDH1 inhibitors for the treatment of tumors
Bayer Pharma Aktiengesellschaft
2-oxothiazole compounds and method of using same for chronic inflammatory disorders
Avexxin
Theoretical studies on the molecular basis of HIV-1RT/NNRTIs interactions.
Chulalongkorn University
Tetrahydroisoquinoline derivatives, pharmaceutical compositions and uses thereof
Boehringer Ingelheim International
Substituted N-phenethyltriazoloneacetamides and use thereof
Bayer Intellectual Property
Reactivators of organophosphorous inhibited acetylcholinesterase
Southwest Research Institute
Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases
Hanmi Pharm.
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
Merck Sharpe & Dohme
Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist.
Pharmacia and Upjohn
Identification and characterization of novel somatostatin antagonists.
Cyenamid Agricultural Research Center
Inhibition studies of porphobilinogen synthase from Escherichia coli differentiating between the two recognition sites.
University of NeuchÂTel
Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.
Berlex
Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists.
Johnson & Johnson Pharmaceutical
Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays.
Universite De La Mediterranee
Small molecule peptidomimetics containing a novel phosphotyrosine bioisostere inhibit protein tyrosine phosphatase 1B and augment insulin action.
Pharmacia
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.
Chemical Diversity
High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II.
Uppsala University
SAR and 3D-QSAR studies on thiadiazolidinone derivatives: exploration of structural requirements for glycogen synthase kinase 3 inhibitors.
Instituto De Quimica Medica (Csic)
First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease.
Instituto De Quimica Medica (Csic)
Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors.
Institut Curie