The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28657320 |
46 |
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 |
28296398 |
73 |
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERa+ Breast Cancer. |
Novartis Institutes For Biomedical Research |
28117994 |
21 |
Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer. |
University of Illinois College of Pharmacy |
27919612 |
4 |
An in-tether sulfoxide chiral center influences the biophysical properties of the N-capped peptides. |
Peking University Shenzhen Graduate School |
28105283 |
6 |
Rational Design of a Boron-Modified Triphenylethylene (GLL398) as an Oral Selective Estrogen Receptor Downregulator. |
Xavier University of Louisiana |
27810243 |
87 |
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators. |
Astrazeneca |
27994732 |
56 |
Development of |
Tokyo Medical and Dental University |
27647375 |
9 |
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C. |
University of Michigan |
27647367 |
36 |
A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptorsa andß. |
Purdue University |
27236015 |
60 |
Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists. |
Daegu-Gyeongbuk Medical Innovation Foundation |
27176944 |
26 |
Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERa and VEGFR-2 as anti-breast cancer agents. |
China Pharmaceutical University |
27407030 |
8 |
Synthesis, antiproliferative and pro-apoptotic activity of 2-phenylindoles. |
Trinity College |
26881908 |
13 |
De Novo Design at the Edge of Chaos. |
Swiss Federal Institute of Technology (Eth) |
27185013 |
10 |
Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator. |
National Institute of Health Sciences |
26905830 |
4 |
Identification of novel estrogen receptor (ER) agonists that have additional and complementary anti-cancer activities via ER-independent mechanism. |
Kyung Hee University |
26897089 |
39 |
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists. |
Vitae Pharmaceuticals |
26896706 |
18 |
Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism. |
German University In Cairo |
26819673 |
55 |
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat. |
Astrazeneca |
26681208 |
21 |
Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer. |
University of Illinois At Chicago |
26764190 |
4 |
Peptide-based inhibitors of protein-protein interactions. |
Wroclaw University of Technology |
26407012 |
80 |
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 |
25992880 |
90 |
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. |
University of Bath |
26183544 |
16 |
Structural development of stabilized helical peptides as inhibitors of estrogen receptor (ER)-mediated transcription. |
National Institute of Health Sciences |
25993269 |
140 |
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) |
26003343 |
10 |
Synthesis and evaluation of tamoxifen derivatives with a long alkyl side chain as selective estrogen receptor down-regulators. |
National Institute of Health Sciences |
25879485 |
60 |
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 |
25941555 |
75 |
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists. |
Merck Research Laboratories |
25790336 |
93 |
Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
Astrazeneca |
25751283 |
79 |
Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities. |
Purdue University |
25706100 |
65 |
2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists. |
TBA |
25559213 |
14 |
Highly selective salicylketoxime-based estrogen receptorß agonists display antiproliferative activities in a glioma model. |
Universit£ |
25121964 |
18 |
3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration. |
Novartis Institutes For Biomedical Research |
24980053 |
153 |
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists. |
Bristol-Myers Squibb |
25369367 |
25 |
ß-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand. |
Trinity College |
25305688 |
41 |
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t. |
Phenex Pharmaceuticals |
24837157 |
2 |
Novel estrogen receptor (ER) modulators containing various hydrophobic bent-core structures. |
Tohoku Pharmaceutical University |
24805199 |
10 |
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 |
24755427 |
107 |
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation. |
Astrazeneca |
24738581 |
81 |
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 |
24630411 |
38 |
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series. |
Merck Research Laboratories |
24708493 |
50 |
Triaryl-substituted Schiff bases are high-affinity subtype-selective ligands for the estrogen receptor. |
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University) |
24630694 |
11 |
Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character. |
The University of Tokyo |
23586645 |
48 |
Thiophene-core estrogen receptor ligands having superagonist activity. |
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University) |
22280402 |
12 |
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer. |
Trinity College |
20812681 |
24 |
Synthesis and biochemical characterization of a series of 17a-perfluoroalkylated estradiols as selective ligands for estrogen receptora. |
Charles University In Prague |
15686893 |
84 |
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 |
14761193 |
11 |
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 |
12139447 |
6 |
(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 |
23079530 |
27 |
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides. |
Pfizer |
23043242 |
29 |
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 |
22652053 |
6 |
Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins. |
Rwth Aachen University |
22647217 |
57 |
Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening. |
East China University of Science and Technology |
22582136 |
8 |
Hydrophobic Interactions Improve Selectivity to ERa for Ben-zothiophene SERMs. |
TBA |
22608920 |
4 |
Synthesis and evaluation of 11ß-(4-substituted phenyl) estradiol analogs: transition from estrogen receptor agonists to antagonists. |
Northeastern University |
22283328 |
28 |
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 |
22405286 |
10 |
Recent advances in the synthesis of raloxifene: a selective estrogen receptor modulator. |
Torrey Pines Institute For Molecular Studies |
21073190 |
135 |
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists. |
Bristol-Myers Squibb |
21218783 |
117 |
Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents. |
Johnson & Johnson Pharmaceutical Research and Development |
20875743 |
90 |
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 |
20598555 |
3 |
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 |
20672822 |
108 |
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 |
20510622 |
142 |
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists. |
Chinese Academy of Sciences |
20553023 |
46 |
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening. |
East China University of Science and Technology |
19863083 |
25 |
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. |
Wyeth Research |
19836949 |
31 |
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 |
19824648 |
19 |
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 |
19321341 |
101 |
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators. |
Bristol-Myers Squibb |
18722119 |
55 |
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 |
15568770 |
4 |
Estrogenic and anticarcinogenic properties of kurarinone, a lavandulyl flavanone from the roots of Sophora flavescens. |
Ghent University |
18318463 |
53 |
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 |
18269232 |
4 |
Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta. |
Universita Di Pisa |
17890084 |
86 |
Androstene-3,5-dienes as ER-beta selective SERMs. |
Merck Research Laboratories |
17448656 |
80 |
Bridged androstenediol analogs as ER-beta selective SERMs. |
Merck Research Laboratories |
17696335 |
8 |
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 |
16309907 |
129 |
Androstenediol analogs as ER-beta-selective SERMs. |
Merck Research Laboratories |
16451049 |
4 |
A selective estrogen receptor modulator for the treatment of hot flushes. |
Eli Lilly |
15887952 |
26 |
Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases. |
University of Southern California |
15293993 |
172 |
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes. |
Abbott Laboratories |
12672240 |
18 |
De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor. |
Signalgene |
12036351 |
31 |
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. |
Pfizer |
15081034 |
76 |
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15080982 |
122 |
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists. |
Abbott Laboratories |
14643316 |
11 |
6-(2-adamantan-2-ylidene-hydroxybenzoxazole)-O-sulfamate: a potent non-steroidal irreversible inhibitor of human steroid sulfatase. |
Novartis Forschungsinstitut |
11459643 |
20 |
Phytoestrogens from the roots of Polygonum cuspidatum (Polygonaceae): structure-requirement of hydroxyanthraquinones for estrogenic activity. |
Kyoto Pharmaceutical University |
10673099 |
34 |
Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives. |
Wyeth-Ayerst Research |
22122563 |
34 |
Diarylpropionitrile (DPN) enantiomers: synthesis and evaluation of estrogen receptorß-selective ligands. |
University of Illinois |
22061644 |
10 |
Investigation of the diastereomerism of dihydrobenzoxathiin SERMs for ER alpha by molecular modeling. |
Zhejiang University |
21937153 |
46 |
Recent progress in synthesis and bioactivity studies of indolizines. |
University of Botswana |
21899328 |
244 |
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 |
21885279 |
31 |
Sulfonamides as selective oestrogen receptorß agonists. |
Pfizer |
21839641 |
2 |
DNA site-specific N3-adenine methylation targeted to estrogen receptor-positive cells. |
University of North Carolina At Wilmington |
21481497 |
12 |
Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes. |
Universit£ |
21510635 |
6 |
Estrogenic activity of chemical constituents from Tephrosia candida. |
National Research Centre |
21381753 |
24 |
Design and evaluation of fragment-like estrogen receptor tetrahydroisoquinoline ligands from a scaffold-detection approach. |
Technische Universiteit Eindhoven |
21247762 |
13 |
Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor. |
Chinese Academy of Sciences |
20527892 |
7 |
Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs. |
Institute of Theoretical Studies Ggmbh |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
20659801 |
6 |
A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements. |
University of Delaware |
16520733 |
8 |
Virtual and biomolecular screening converge on a selective agonist for GPR30. |
University of New Mexico Health Sciences Center |
20669983 |
1 |
Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells. |
Xavier University of Louisiana |
20621492 |
6 |
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha. |
Instituto PolitéCnico Nacional 2508 |
19561619 |
5 |
Bioactivity-guided mapping and navigation of chemical space. |
Institut FüR Molekulare Physiologie |
20638278 |
145 |
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. |
Phenex Pharmaceuticals |
20493686 |
10 |
New estrogenic compounds isolated from Broussonetia kazinoki. |
Sookmyung Women'S University |
20462217 |
17 |
Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery. |
Pfizer |
20430618 |
21 |
Optimisation of a pyrazole series of progesterone antagonists; Part 1. |
Pfizer |
20408553 |
27 |
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines. |
Pfizer |
20408532 |
3 |
Synthesis and evaluation of 17alpha-arylestradiols as ligands for estrogen receptor alpha and beta. |
Academy of Sciences of The Czech Republic |
20144545 |
19 |
LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators. |
The University of Tokyo |
19705860 |
2 |
Isoflavonoids from Erythrina poeppigiana: evaluation of their binding affinity for the estrogen receptor. |
University of Athens |
19366247 |
239 |
Identification and structure-activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms. |
Johnson & Johnson Pharmaceutical Research & Development |
20031420 |
13 |
Click synthesis of estradiol-cyclodextrin conjugates as cell compartment selective estrogens. |
University of Illinois At Chicago |
19954971 |
40 |
Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer. |
Sumitomo Chemical |
19286283 |
22 |
Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta. |
University of Illinois |
19394116 |
14 |
Phenethyl pyridines with non-polar internal substituents as selective ligands for estrogen receptor beta. |
University of Illinois |
19606870 |
53 |
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs). |
Merck Research Laboratories |
19394231 |
2 |
Steroidal bivalent ligands for the estrogen receptor: design, synthesis, characterization and binding affinities. |
University of Illinois At Urbana-Champaign |
19359182 |
2 |
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 |
19356928 |
5 |
Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor beta. |
University of Pittsburgh |
19239259 |
66 |
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration. |
Pfizer |
19128016 |
11 |
Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta. |
Universita Di Pisa |
19014882 |
3 |
Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity. |
University of Illinois |
18976929 |
33 |
Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor. |
University of Illinois At Urbana-Champaign |
18942824 |
2 |
Cobalt-alkyne complexes with imidazoline ligands as estrogenic carriers: synthesis and pharmacological investigations. |
Freie Universitat Berlin |
18835176 |
32 |
Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators. |
Trinity College |
18785725 |
277 |
Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding. |
University of Illinois At Urbana-Champaign |
18760603 |
2 |
Promising core structure for nuclear receptor ligands: design and synthesis of novel estrogen receptor ligands based on diphenylamine skeleton. |
Tohoku Pharmaceutical University |
18722117 |
24 |
Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands. |
Glaxosmithkline |
18457385 |
41 |
Recent developments in fragment-based drug discovery. |
Astex Therapeutics |
16499324 |
2 |
Bioactive compounds from Peperomia pellucida. |
Chinese Academy of Sciences |
16441086 |
4 |
Isoflavonoids with antiestrogenic activity from Millettia pachycarpa. |
Meijo University |
12502307 |
6 |
Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis. |
Université |
11141112 |
2 |
Three new arylobenzofurans from Onobrychis ebenoides and evaluation of their binding affinity for the estrogen receptor. |
University of Athens |
18038968 |
26 |
(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 |
17918820 |
6 |
Target specific virtual screening: optimization of an estrogen receptor screening platform. |
Trinity College |
17902637 |
2 |
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 |
17574424 |
28 |
Aza analogues of equol: novel ligands for estrogen receptor beta. |
Chinese Academy of Sciences |
17560105 |
6 |
Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. |
University of Illinois |
17482463 |
34 |
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety. |
Eli Lilly |
17379515 |
9 |
Synthesis, characterization, and estrogen receptor binding affinity of flavone-, indole-, and furan-estradiol conjugates. |
Université |
17289385 |
50 |
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha. |
Merck Research Laboratories |
17275315 |
1 |
Synthesis, structure, and estrogenic activity of 4-amino-3-(2-methylbenzyl)coumarins on human breast carcinoma cells. |
Equipe De Chimie ThéRapeutique |
17188490 |
24 |
ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives. |
Wyeth Research |
17049855 |
36 |
Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones. |
Wyeth Research |
16942012 |
56 |
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) |
16884312 |
3 |
Synthesis of anthranylaldoxime derivatives as estrogen receptor ligands and computational prediction of binding modes. |
Università |
16815012 |
20 |
Tetrahydrofluorenones with conformationally restricted side chains as selective estrogen receptor beta ligands. |
Merck Research Laboratories |
16777408 |
89 |
Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists. |
Merck Research Laboratories |
16730987 |
106 |
Estrogen receptor beta-subtype selective tetrahydrofluorenones: use of a fused pyrazole as a phenol bioisostere. |
Merck Research Laboratories |
16722623 |
12 |
Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness. |
Johnson & Johnson Pharmaceutical Research & Development |
16632357 |
89 |
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands. |
Merck Research Laboratories |
16412638 |
126 |
6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists. |
Merck Research Laboratories |
16300947 |
60 |
Substituted 4-hydroxyphenyl sulfonamides as pathway-selective estrogen receptor ligands. |
Wyeth Research |
16219463 |
34 |
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands. |
Pfizer |
16203138 |
26 |
Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms. |
Merck Research Laboratories |
16162002 |
51 |
Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands. |
University of California |
16098741 |
50 |
ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives. |
Wyeth Research |
15943471 |
140 |
ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity. |
Wyeth Research |
15911283 |
62 |
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity. |
Merck Research Laboratories |
15911274 |
26 |
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators. |
Chinese Academy of Sciences |
15876535 |
46 |
Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones. |
Wyeth Research |
15745820 |
42 |
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs. |
Merck Research Laboratories |
15713417 |
40 |
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. |
Chinese Academy of Sciences |
15713407 |
52 |
Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold. |
Ligand Pharmaceuticals |
15664843 |
14 |
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans. |
Merck Research Laboratories |
15658860 |
14 |
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 |
15588074 |
43 |
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 |
15582421 |
54 |
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers. |
Merck Research Laboratories |
15456246 |
251 |
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. |
Wyeth Research |
15341953 |
46 |
7-Substituted 2-phenyl-benzofurans as ER beta selective ligands. |
Wyeth Research |
15225686 |
34 |
Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains. |
Merck Research Laboratories |
15225685 |
34 |
Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains. |
Merck Research Laboratories |
15203156 |
20 |
Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins. |
Merck Research Laboratories |
15203155 |
26 |
Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains. |
Merck Research Laboratories |
15125925 |
110 |
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs. |
Merck Research Laboratories |
15125923 |
60 |
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists. |
Pfizer |
15109649 |
44 |
Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs. |
Merck Research Laboratories |
15084115 |
32 |
Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators. |
Merck Research Laboratories |
15006374 |
54 |
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity. |
Merck Research Laboratories |
14980690 |
12 |
Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree! |
Merck Research Laboratories |
14643309 |
12 |
B-ring unsaturated estrogens: biological evaluation of 17alpha-Dihydroequilein and novel B-Nor-6-thiaequilenins as tissue selective estrogens. |
Eli Lilly |
14592514 |
8 |
Utility of boron clusters for drug design. Relation between estrogen receptor binding affinity and hydrophobicity of phenols bearing various types of carboranyl groups. |
Tohoku Pharmaceutical University |
12954056 |
14 |
Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process. |
Università |
12877579 |
6 |
Identification of"latent hits" in compound screening collections. |
Organon Laboratories |
12824043 |
40 |
Constrained phytoestrogens and analogues as ERbeta selective ligands. |
Wyeth Research |
12749898 |
11 |
A novel estrogen receptor ligand template. |
Bayer |
12749895 |
37 |
Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs). |
Eli Lilly |
12668015 |
6 |
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 |
12646017 |
1 |
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents. |
The Feinberg School of Medicine of Northwestern University |
12565955 |
33 |
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs). |
Merck Research Laboratories |
12459017 |
132 |
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta. |
Glaxosmithkline |
12431063 |
8 |
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 |
11965371 |
4 |
Synthesis of a novel fluorescent probe for estrogen receptor. |
Abbott Laboratories |
11708925 |
44 |
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues. |
University of Illinois |
11549460 |
16 |
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 |
11459665 |
36 |
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor. |
Glaxo Wellcome Research and Development |
31987694 |
40 |
Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening. |
Trinity College |
31879182 |
28 |
Bisphenol AF: Halogen bonding effect is a major driving force for the dual ER?-agonist and ER?-antagonist activities. |
Kyushu University |
11356100 |
15 |
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
Wyeth-Ayerst Research |
32551022 |
23 |
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer. |
Genentech |
31980362 |
15 |
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 |
32435424 |
12 |
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR. |
University of Naples "Federico Ii |
32163286 |
1 |
Antiausterity Activity of Secondary Metabolites from the Roots of |
University of Innsbruck |
27503683 |
12 |
Non-canonical modulators of nuclear receptors. |
Vitae Pharmaceuticals |
27529700 |
6 |
Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD). |
Xavier University of Louisiana |
30732944 |
13 |
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha. |
Genentech |
30657313 |
204 |
Discovery of Potent, Selective, and Orally Bioavailable Estrogen-Related Receptor-? Inverse Agonists To Restore the Sodium Iodide Symporter Function in Anaplastic Thyroid Cancer. |
Daegu-Gyeongbuk Medical Innovation Foundation |
31940200 |
62 |
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. |
Genomics Institute of The Novartis Research Foundation (Gnf) |
30731397 |
11 |
Structure-based drug design, synthesis, In vitro, and In vivo biological evaluation of indole-based biomimetic analogs targeting estrogen receptor-? inhibition. |
The British University In Egypt |
31129450 |
72 |
Estrogen signaling: An emanating therapeutic target for breast cancer treatment. |
Indian Institute of Technology (Bhu) |
10447957 |
5 |
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 |
30940565 |
93 |
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton. |
The University of Tokyo |
31311734 |
30 |
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927. |
Genentech |
10229620 |
3 |
Potent estrogenic agonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore. |
University of Tokyo |
32292542 |
6 |
Selective Estrogen Receptor Degraders for the Potential Treatment of Cancer. |
Usona Institute |
32292540 |
8 |
Cereblon Based Immunomodulatory Therapeutics. |
Usona Institute |
29741891 |
54 |
A-C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions. |
Concordia University Wisconsin |
30640465 |
57 |
Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists. |
Astrazeneca |
31288128 |
6 |
Boron in drug design: Recent advances in the development of new therapeutic agents. |
S£O Paulo State University |
31099568 |
18 |
Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index. |
Helmholtz-Zentrum Dresden-Rossendorf |
31746603 |
34 |
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer. |
University of Illinois At Chicago |
30888810 |
48 |
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
Sun Yat-Sen University |
30939353 |
2 |
Exploring the PROTAC degron candidates: OBHSA with different side chains as novel selective estrogen receptor degraders (SERDs). |
Wuhan University |
30655946 |
27 |
Maximizing ER-? Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927. |
Seragon Pharmaceuticals |
30587451 |
63 |
Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft. |
Seragon Pharmaceuticals |
30384047 |
16 |
Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ER? and VEGFR-2. |
China Pharmaceutical University |
31729873 |
43 |
Structure-Based and Property-Driven Optimization of |
Global Discovery Chemistry |
31721572 |
27 |
Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3 |
Sanofi |
31461285 |
1 |
Myrmenaphthol A, Isolated from a Hawaiian Sponge of the Genus |
University of Hawaii At Manoa |
31620239 |
19 |
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
Astrazeneca |
31620216 |
5 |
PROTAC-Mediated Degradation of Estrogen Receptor in the Treatment of Cancer. |
Usona Institute |
26822566 |
1 |
Symmetric 4,4'-(piperidin-4-ylidenemethylene)bisphenol derivatives as novel tunable estrogen receptor (ER) modulators. |
Tohoku Pharmaceutical University |
26795112 |
6 |
Structural features underlying raloxifene's biophysical interaction with bone matrix. |
Lilly Research Laboratories |
26613635 |
23 |
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids. |
Mcgill University |
24360824 |
3 |
4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors. |
Northeastern University |
24315190 |
21 |
Probing the human estrogen receptor-? binding requirements for phenolic mono- and di-hydroxyl compounds: a combined synthesis, binding and docking study. |
Marquette University |
23880359 |
19 |
3D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors. |
University of Siena |
23786452 |
25 |
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
Georgia Institute of Technology |
23608764 |
23 |
Discovery of natural estrogen receptor modulators with structure-based virtual screening. |
East China University of Science and Technology |
15771467 |
34 |
Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling. |
Glaxosmithkline Research & Development |
30144697 |
66 |
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs). |
Marquette University |
29641206 |
11 |
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 |
29207335 |
6 |
Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives. |
American University of Ras Al Khaimah |
30078609 |
16 |
Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm. |
Mcgill University |
30025900 |
43 |
Recent advances in peptidomimetics antagonists targeting estrogen receptor ?-coactivator interaction in cancer therapy. |
Peking University Shenzhen Graduate School |
29605809 |
19 |
Success stories of natural product-based hybrid molecules for multi-factorial diseases. |
Punjabi University |
29587221 |
31 |
Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ER?/VEGFR-2 ligands with anti-breast cancer activity. |
China Pharmaceutical University |
29525335 |
14 |
Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton. |
Nagasaki University |
28426931 |
59 |
Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ER? and ER? Activity. |
Trinity College |
30053783 |
121 |
Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer. |
Wuhan University |
29424542 |
138 |
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
Astrazeneca |
28812892 |
4 |
DESIGNER Extracts as Tools to Balance Estrogenic and Chemopreventive Activities of Botanicals for Women's Health. |
Hallertauer Hopfenveredelung |
29198894 |
11 |
Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators. |
Central University of Punjab |
28319389 |
31 |
Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17?-Hydroxysteroid Dehydrogenase Type 2. |
University of Basel |
30086626 |
32 |
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 |
29869503 |
4 |
Dehydrodiconiferyl Alcohol Inhibits Osteoclast Differentiation and Ovariectomy-Induced Bone Loss through Acting as an Estrogen Receptor Agonist. |
Seoul National University |
29407951 |
11 |
Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-?). |
Central University of Punjab |
29348811 |
17 |
Disconnecting the Estrogen Receptor Binding Properties and Antimicrobial Properties of Parabens through 3,5-Substitution. |
Longwood University |
29152041 |
28 |
Selective Estrogen Receptor Degraders (SERDs): A Promising Treatment to Overcome Resistance to Endocrine Therapy in ER?-Positive Breast Cancer. |
Therachem Research Medilab (India) |
28942113 |
34 |
Novel SERMs based on 3-aryl-4-aryloxy-2H-chromen-2-one skeleton - A possible way to dual ER?/VEGFR-2 ligands for treatment of breast cancer. |
China Pharmaceutical University |
28759875 |
30 |
An overview of benzo[b]thiophene-based medicinal chemistry. |
Jain University |
28735214 |
54 |
Indazole-based ligands for estrogen-related receptor ? as potential anti-diabetic agents. |
Janssen Research and Development |
28886996 |
23 |
A prodrug design for improved oral absorption and reduced hepatic interaction. |
Evestra |
28882502 |
27 |
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents. |
Kyushu University |
28506582 |
11 |
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 |
28937774 |
107 |
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. |
Astrazeneca |
29300474 |
45 |
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists. |
Pfizer |
29562737 |
74 |
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 |
29045135 |
12 |
Structural Basis of Inhibition of ER?-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides. |
Shenzhen Graduate School of Peking University |
28400239 |
9 |
Efficient synthesis of a multi-substituted diphenylmethane skeleton as a steroid mimetic. |
National Institute of Health Sciences |
27908539 |
20 |
Design, synthesis, molecular docking, anti-Proteus mirabilis and urease inhibition of new fluoroquinolone carboxylic acid derivatives. |
Minia University |
27250740 |
15 |
Electrostatic Control of Isoform Selective Inhibitor Binding in Nitric Oxide Synthase. |
University of California Irvine |
15123280 |
12 |
Systems-based design of bi-ligand inhibitors of oxidoreductases: filling the chemical proteomic toolbox. |
Triad Therapeutics |
15123247 |
29 |
Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors. |
Cyclacel |
14700626 |
35 |
Inhibitor specificity via protein dynamics: insights from the design of antibacterial agents targeted against thymidylate synthase. |
UniversitÀ |
19147350 |
264 |
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: part 2. |
Schering-Plough Research Institute |
17985858 |
27 |
Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1. |
Georgetown University Medical Center |
16876407 |
52 |
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors. |
Gnf |
16828557 |
19 |
Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer. |
University of Tennessee Health Science Center |
15857115 |
22 |
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. |
Karo Bio |
16125392 |
15 |
Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors. |
Ohio State University |
11881998 |
32 |
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) |
8355247 |
34 |
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 |
1712395 |
43 |
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones. |
Boehringer Ingelheim Pharmaceuticals |