The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28363748 |
8 |
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives. |
Takeda Pharmaceutical |
28051871 |
100 |
Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
Instituto De Qu£Mica M£Dica (Iqm-Csic) |
27836399 |
26 |
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists. |
Bristol-Myers Squibb Research and Development |
27810243 |
87 |
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators. |
Astrazeneca |
27994732 |
56 |
Development of |
Tokyo Medical and Dental University |
27994731 |
3 |
Identification of Triptophenolide from |
Chinese Academy of Medical Science |
27717544 |
75 |
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors. |
Integral Biosciences |
27665178 |
42 |
Development of 6-arylcoumarins as nonsteroidal progesterone antagonists. Structure-activity relationships and fluorescence properties. |
Ochanomizu University |
27301368 |
4 |
Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. |
Cardiff University |
26819671 |
51 |
Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs). |
Glaxosmithkline |
26965862 |
3 |
7-Substituted umbelliferone derivatives as androgen receptor antagonists for the potential treatment of prostate and breast cancer. |
Cardiff University |
26683992 |
25 |
2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy. |
Eli Lilly |
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 |
26295173 |
25 |
Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists. |
Ochanomizu University |
26288692 |
37 |
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer. |
Bristol-Myers Squibb Research and Development |
26305181 |
13 |
Discovery of Potent 17ß-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors. |
University of Arizona |
26218343 |
76 |
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site. |
Eli Lilly |
26046313 |
20 |
Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists. |
Alla Chem |
25978072 |
53 |
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists. |
TBA |
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 |
25706100 |
65 |
2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists. |
TBA |
25591066 |
23 |
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer. |
University of Maryland |
25646649 |
20 |
Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators. |
University of Gothenburg |
25862209 |
31 |
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I. |
Takeda Pharmaceutical |
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 |
25025737 |
37 |
Discovery of 1H-indole-2-carboxamides as novel inhibitors of the androgen receptor binding function 3 (BF3). |
University of British Columbia |
24980053 |
153 |
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists. |
Bristol-Myers Squibb |
25440884 |
2 |
Synthetic derivatives of aromatic abietane diterpenoids and their biological activities. |
Universidad De Valencia |
25305688 |
41 |
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t. |
Phenex Pharmaceuticals |
25187277 |
136 |
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists. |
Takeda Pharmaceutical |
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 |
24726305 |
3 |
Preliminary investigations into triazole derived androgen receptor antagonists. |
Deakin University |
24630411 |
38 |
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series. |
Merck Research Laboratories |
24527807 |
82 |
1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators. |
Pfizer |
24446728 |
30 |
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design. |
Eli Lilly |
24157365 |
23 |
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists. |
Pfizer |
24900588 |
25 |
Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists. |
Tokyo Medical and Dental University |
24044500 |
2 |
Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators. |
National Cancer Institute-Frederick |
23953070 |
146 |
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists. |
Ironwood Pharmaceuticals |
23916594 |
92 |
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists. |
Bristol-Myers Squibb |
23958516 |
61 |
Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists. |
Takeda Pharmaceutical |
23777778 |
101 |
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists. |
Merck Research Laboratories |
23768907 |
6 |
Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERa-selective antagonist. |
The University of Tokyo |
23727044 |
6 |
Discovery of non-LBD inhibitor for androgen receptor by structure-guide design. |
Korea Research Institute of Chemical Technology |
23713567 |
13 |
Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer. |
University of Maryland |
23611768 |
34 |
The systematic structure-activity relationship to predict how flavones bind to human androgen receptor for their antagonistic activity. |
Meijo University |
23466225 |
2 |
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer. |
Astrazeneca |
23462715 |
25 |
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange. |
The University of Tokyo |
23199477 |
47 |
Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists. |
Takeda Pharmaceutical |
23432095 |
160 |
Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17ß-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. |
Vanderbilt University School of Medicine |
23301637 |
63 |
Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives. |
University of British Columbia |
22280402 |
12 |
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer. |
Trinity College |
20727743 |
64 |
Discovery of quinolines as selective glucocorticoid receptor agonists. |
Bayer Schering Pharma |
20469868 |
176 |
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists. |
Glaxosmithkline |
19856921 |
21 |
Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. |
Acadia Pharmaceuticals |
19664922 |
35 |
2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists. |
Glaxosmithkline |
18952422 |
5 |
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist. |
Glaxosmithkline |
11150172 |
8 |
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
Schering |
23079530 |
27 |
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides. |
Pfizer |
22897611 |
2 |
Discovery of diarylhydantoins as new selective androgen receptor modulators. |
Galapagos, Parc Biocitech |
22866979 |
19 |
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy. |
Pfizer |
22746350 |
41 |
Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators. |
University of Eastern Finland |
22507964 |
17 |
Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer. |
Perelman School of Medicine University of Pennsylvania |
22377517 |
15 |
Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists. |
Pfizer |
22310230 |
2 |
Methoxychalcone inhibitors of androgen receptor translocation and function. |
National Cancer Institute-Bethesda |
21073190 |
135 |
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists. |
Bristol-Myers Squibb |
21050768 |
20 |
Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer. |
Chugai Pharmaceutical |
21036041 |
22 |
Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs). |
Radius Health |
20888766 |
50 |
Novel selective anti-androgens with a diphenylpentane skeleton. |
The University of Tokyo |
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 |
20672820 |
92 |
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists. |
Pfizer |
20638844 |
25 |
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists. |
Pfizer |
20584610 |
90 |
Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists. |
Bristol-Myers Squibb |
20510622 |
142 |
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists. |
Chinese Academy of Sciences |
20381361 |
43 |
Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists. |
Chugai Pharmaceutical |
20355713 |
3 |
Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget. |
University of Illinois |
19863083 |
25 |
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. |
Wyeth Research |
20047280 |
174 |
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators. |
Bristol-Myers Squibb |
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 |
18504132 |
51 |
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists. |
Wyeth Research |
18400499 |
53 |
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity. |
Ligand Pharmaceuticals |
18513967 |
103 |
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines. |
Ligand Pharmaceuticals |
18032610 |
4 |
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. |
Ligand Pharmaceuticals |
17911242 |
1 |
A surface on the androgen receptor that allosterically regulates coactivator binding. |
University of California |
17606915 |
4 |
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. |
The Scripps Research Institute |
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 |
18442912 |
90 |
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones. |
Ligand Pharmaceuticals |
18291644 |
62 |
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists. |
Bristol-Myers Squibb Pharmaceutical Research and Development |
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 |
17064916 |
61 |
Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships. |
Chugai Pharmaceutical |
16309907 |
129 |
Androstenediol analogs as ER-beta-selective SERMs. |
Merck Research Laboratories |
16250653 |
22 |
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
Universit£ |
15771445 |
22 |
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors. |
University of Ferrara |
15456242 |
30 |
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor. |
The Pennsylvania State University |
15293993 |
172 |
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes. |
Abbott Laboratories |
14613328 |
10 |
Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate. |
University of Colorado |
12238914 |
48 |
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists. |
Women'S Health Research Institute |
12036351 |
31 |
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. |
Pfizer |
10212133 |
93 |
5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification. |
Ligand Pharmaceuticals |
9925725 |
9 |
Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071). |
Ligand Pharmaceuticals |
9484511 |
111 |
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. |
Ligand Pharmaceuticals |
8627601 |
169 |
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether. |
Ligand Pharmaceuticals |
15081005 |
30 |
Novel pyrrole-containing progesterone receptor modulators. |
Wyeth Research |
15080982 |
122 |
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists. |
Abbott Laboratories |
12781198 |
108 |
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore. |
Ligand Pharmaceuticals |
12781197 |
59 |
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators. |
Ligand Pharmaceuticals |
10743938 |
103 |
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines. |
Ligand Pharmaceuticals |
10340624 |
72 |
4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists. |
Ligand Pharmaceuticals |
9873735 |
111 |
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators. |
Ligand Pharmaceuticals |
22391033 |
69 |
Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists. |
Takeda Pharmaceutical |
22197140 |
15 |
Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer. |
Pfizer |
22094279 |
75 |
Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists. |
Takeda Pharmaceutical |
22074142 |
89 |
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists. |
Takeda Pharmaceutical |
22047606 |
29 |
Targeting the binding function 3 (BF3) site of the human androgen receptor through virtual screening. |
University of British Columbia |
21936524 |
21 |
Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. |
Pfizer |
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 |
21916484 |
41 |
6-arylcoumarins as novel nonsteroidal type progesterone antagonists: an example with receptor-binding-dependent fluorescence. |
Ochanomizu University |
21831636 |
75 |
Pantolactams as androgen receptor antagonists for the topical suppression of sebum production. |
Pfizer |
21846139 |
12 |
Inhibitors of androgen receptor activation function-2 (AF2) site identified through virtual screening. |
University of British Columbia |
21506597 |
6 |
Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets. |
The University of Tennessee |
21324689 |
74 |
Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation. |
Ligand Pharmaceuticals |
21316964 |
108 |
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists. |
Ligand Pharmaceuticals |
24900290 |
7 |
Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140 |
TBA |
24900294 |
72 |
Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine Fibroids |
TBA |
21115247 |
64 |
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity. |
Ligand Pharmaceuticals |
20826091 |
6 |
20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth. |
UniversitäT Leipzig |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
20638278 |
145 |
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. |
Phenex Pharmaceuticals |
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 |
20226658 |
5 |
Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay. |
Meijo University |
20144545 |
19 |
LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators. |
The University of Tokyo |
19954971 |
40 |
Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer. |
Sumitomo Chemical |
19616429 |
32 |
Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists. |
Glaxosmithkline |
19595590 |
49 |
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists. |
Glaxosmithkline |
19606870 |
53 |
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs). |
Merck Research Laboratories |
19592245 |
11 |
Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay. |
Meijo University |
19432422 |
16 |
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. |
Gtx |
19286380 |
49 |
Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production. |
Pfizer |
19239259 |
66 |
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration. |
Pfizer |
19201190 |
56 |
4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production. |
Pfizer |
18707892 |
2 |
Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring. |
Tohoku Pharmaceutical University |
18571420 |
71 |
4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
The University of Tokyo |
18553958 |
28 |
A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochromeno[3,4-f]quinoline. |
Ligand Pharmaceuticals |
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 |
17827000 |
6 |
(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production. |
Pfizer |
17804229 |
31 |
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. |
Chugai Pharmaceutical |
17766112 |
22 |
Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production. |
Pfizer |
17764935 |
32 |
Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production. |
Pfizer |
17703938 |
55 |
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones. |
Ligand Pharmaceuticals |
17681796 |
21 |
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist. |
Wyeth Research |
17574413 |
24 |
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators. |
Bristol-Myers Squibb Research and Development |
17553679 |
148 |
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators. |
Ligand Pharmaceuticals |
17292608 |
48 |
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators. |
Pharmaceutical Research Institute |
17197181 |
3 |
Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold. |
Johnson & Johnson Pharmaceutical Research and Development |
17149866 |
4 |
Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist. |
Orebro University |
16019211 |
14 |
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities. |
The University of Tokyo |
15603960 |
84 |
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15603938 |
54 |
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15546739 |
60 |
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15509168 |
10 |
Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera. |
University of Colorado |
15081010 |
66 |
Discovery of novel nonsteroidal glucocorticoid receptor modulators. |
Abbott Laboratories |
12954062 |
140 |
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators. |
Ligand Pharmaceuticals |
12873487 |
5 |
Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor. |
The University of Tokyo |
12620078 |
132 |
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines. |
Abbott Laboratories |
11520196 |
81 |
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity. |
Abbott Laboratories |
32847363 |
66 |
Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer. |
Gifu Pharmaceutical University |
11356108 |
3 |
Homology modeling using multiple molecular dynamics simulations and docking studies of the human androgen receptor ligand binding domain bound to testosterone and nonsteroidal ligands. |
The University of Tennessee Health Science Center |
27503683 |
12 |
Non-canonical modulators of nuclear receptors. |
Vitae Pharmaceuticals |
27437082 |
12 |
Identification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3?-Imidazole Carbamate. |
University of Maryland |
27563404 |
36 |
Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer. |
University of Pittsburgh |
10743937 |
66 |
Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines. |
Ligand Pharmaceuticals |
30525603 |
162 |
New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity. |
University of Tennessee Health Science Center |
31274313 |
95 |
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633). |
Oric Pharmaceuticals |
31940200 |
62 |
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. |
Genomics Institute of The Novartis Research Foundation (Gnf) |
10230629 |
69 |
Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone. |
Ligand Pharmaceuticals |
10230628 |
95 |
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one. |
Ligand Pharmaceuticals |
29400967 |
136 |
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. |
Bristol-Myers Squibb |
31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
9871534 |
95 |
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone. |
Ligand Pharmaceuticals |
31271960 |
1 |
Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines. |
The Czech Academy of Sciences |
9784110 |
81 |
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists. |
Ligand Pharmaceuticals |
30925341 |
4 |
Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer. |
Sichuan University and Collaborative Innovation Center For Biotherapy |
9464360 |
145 |
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists. |
Ligand Pharmaceuticals |
26568144 |
8 |
Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia. |
Eli Lilly |
25062331 |
81 |
Discovery of small-molecule inhibitors selectively targeting the DNA-binding domain of the human androgen receptor. |
University of British Columbia |
30193215 |
20 |
Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor. |
Vancouver Prostate Centre (Vpc) |
30189396 |
38 |
5'-Chloro-2,2'-dihydroxychalcone and related flavanoids as treatments for prostate cancer. |
Kanazawa University |
30144697 |
66 |
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs). |
Marquette University |
28594553 |
10 |
Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands. |
National Institute of Health Sciences |
29424542 |
138 |
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
Astrazeneca |
30091920 |
113 |
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101). |
Oric Pharmaceuticals |
30034593 |
58 |
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton. |
The University of Tokyo |
29407970 |
1 |
High anticancer potency on tumor cells of dehydroabietylamine Schiff-base derivatives and a copper(II) complex. |
Nanjing Forestry University |
29117897 |
3 |
Exploring the tetrahydroisoquinoline thiohydantoin scaffold blockade the androgen receptor as potent anti-prostate cancer agents. |
China Pharmaceutical University |
28757062 |
6 |
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5?-androst-17?-amide derivatives as dual 5?-reductase inhibitors and androgen receptor antagonists. |
China Pharmaceutical University |
28043796 |
84 |
Discovery of new selective glucocorticoid receptor agonist leads. |
Bayer Pharma |
28696695 |
77 |
Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators. |
Pfizer |
29300474 |
45 |
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists. |
Pfizer |
28478926 |
2 |
Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. |
Chinese Academy of Sciences |
28454849 |
48 |
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate. |
Takeda Pharmaceutical |
28385503 |
19 |
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer. |
Drexel University College of Medicine |
26878082 |
196 |
An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy. |
University of Bonn |
28411406 |
16 |
Discovery of novel 2-substituted-4-(2-fluorophenoxy) pyridine derivatives possessing pyrazolone and triazole moieties as dual c-Met/VEGFR-2 receptor tyrosine kinase inhibitors |
China Pharmaceutical University |
12237342 |
2 |
High affinity antagonists of the vanilloid receptor. |
National Cancer Institute-Bethesda |
8935801 |
586 |
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
Janssen Research Foundation |
16216042 |
10 |
Synthesis and biological evaluation of novel EG5 inhibitors. |
University of Leipzig |
1840645 |
85 |
Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. |
University of Toronto |
16990005 |
11 |
Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands. |
Johnson & Johnson Pharmaceutical |
15013001 |
10 |
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains. |
Glaxosmithkline |