233 articles for thisTarget
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Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives.
Takeda Pharmaceutical
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)
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
Bristol-Myers Squibb Research And Development
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.
Astrazeneca
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
Integral Biosciences
Development of 6-arylcoumarins as nonsteroidal progesterone antagonists. Structure-activity relationships and fluorescence properties.
Ochanomizu University
Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
Cardiff University
Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).
Glaxosmithkline
7-Substituted umbelliferone derivatives as androgen receptor antagonists for the potential treatment of prostate and breast cancer.
Cardiff University
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
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
Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists.
Ochanomizu University
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
Bristol-Myers Squibb Research And Development
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
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
Eli Lilly
Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.
Alla Chem
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
TBA
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Seragon Pharmaceuticals
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists.
TBA
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
University Of Maryland
Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.
University Of Gothenburg
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I.
Takeda Pharmaceutical
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 1H-indole-2-carboxamides as novel inhibitors of the androgen receptor binding function 3 (BF3).
University Of British Columbia
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Bristol-Myers Squibb
Synthetic derivatives of aromatic abietane diterpenoids and their biological activities.
Universidad De Valencia
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
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
Preliminary investigations into triazole derived androgen receptor antagonists.
Deakin University
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Merck Research Laboratories
1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators.
Pfizer
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
Eli Lilly
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.
Pfizer
Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists.
Tokyo Medical And Dental University
Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators.
National Cancer Institute-Frederick
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.
Ironwood Pharmaceuticals
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.
Bristol-Myers Squibb
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
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Merck Research Laboratories
Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERa-selective antagonist.
The University Of Tokyo
Discovery of non-LBD inhibitor for androgen receptor by structure-guide design.
Korea Research Institute Of Chemical Technology
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
The systematic structure-activity relationship to predict how flavones bind to human androgen receptor for their antagonistic activity.
Meijo University
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
Astrazeneca
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.
The University Of Tokyo
Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
Takeda Pharmaceutical
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
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
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer.
Trinity College
Discovery of quinolines as selective glucocorticoid receptor agonists.
Bayer Schering Pharma
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.
Glaxosmithkline
Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators.
Acadia Pharmaceuticals
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
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Glaxosmithkline
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
Schering
Discovery of diarylhydantoins as new selective androgen receptor modulators.
Galapagos, Parc Biocitech
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy.
Pfizer
Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators.
University Of Eastern Finland
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
Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists.
Pfizer
Methoxychalcone inhibitors of androgen receptor translocation and function.
National Cancer Institute-Bethesda
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.
Bristol-Myers Squibb
Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
Chugai Pharmaceutical
Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs).
Radius Health
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
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.
Pfizer
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
Pfizer
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
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
Chinese Academy Of Sciences
Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
Chugai Pharmaceutical
Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.
University Of Illinois
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.
Wyeth Research
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.
Bristol-Myers Squibb
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
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
Wyeth Research
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
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.
Ligand Pharmaceuticals
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
Ligand Pharmaceuticals
A surface on the androgen receptor that allosterically regulates coactivator binding.
University Of California
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.
The Scripps Research Institute
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
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
Ligand Pharmaceuticals
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research And Development
Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships.
Chugai Pharmaceutical
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
Universit£
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
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.
The Pennsylvania State University
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
Abbott Laboratories
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
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
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
Pfizer
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
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
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
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
Ligand Pharmaceuticals
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Abbott Laboratories
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
Ligand Pharmaceuticals
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
Ligand Pharmaceuticals
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.
Ligand Pharmaceuticals
4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
Ligand Pharmaceuticals
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.
Ligand Pharmaceuticals
Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
Takeda Pharmaceutical
Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer.
Pfizer
Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
Takeda Pharmaceutical
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
Targeting the binding function 3 (BF3) site of the human androgen receptor through virtual screening.
University Of British Columbia
Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
Pfizer
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
6-arylcoumarins as novel nonsteroidal type progesterone antagonists: an example with receptor-binding-dependent fluorescence.
Ochanomizu University
Pantolactams as androgen receptor antagonists for the topical suppression of sebum production.
Pfizer
Inhibitors of androgen receptor activation function-2 (AF2) site identified through virtual screening.
University Of British Columbia
Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
The University Of Tennessee
Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.
Ligand Pharmaceuticals
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.
Ligand Pharmaceuticals
Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140
TBA
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.
Ligand Pharmaceuticals
20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth.
UniversitäT Leipzig
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical And Public Health Institute
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
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
Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.
Meijo University
LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.
The University Of Tokyo
Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.
Sumitomo Chemical
Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.
Glaxosmithkline
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
Glaxosmithkline
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Merck Research Laboratories
Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.
Meijo University
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
Gtx
Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
Pfizer
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.
Pfizer
4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Pfizer
Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring.
Tohoku Pharmaceutical University
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
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
(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
(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.
Pfizer
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.
Chugai Pharmaceutical
Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.
Pfizer
Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.
Pfizer
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.
Ligand Pharmaceuticals
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
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
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
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
Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold.
Johnson & Johnson Pharmaceutical Research And Development
Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist.
Orebro University
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities.
The University Of Tokyo
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
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
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
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
Ligand Pharmaceuticals
Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.
The University Of Tokyo
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
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Abbott Laboratories
Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer.
Gifu Pharmaceutical University
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
Identification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3?-Imidazole Carbamate.
University Of Maryland
Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer.
University Of Pittsburgh
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
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
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
Oric Pharmaceuticals
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute Of The Novartis Research Foundation (Gnf)
Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.
Ligand Pharmaceuticals
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
Ligand Pharmaceuticals
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Bristol-Myers Squibb
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
Ligand Pharmaceuticals
Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines.
The Czech Academy Of Sciences
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.
Ligand Pharmaceuticals
Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer.
Sichuan University And Collaborative Innovation Center For Biotherapy
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.
Ligand Pharmaceuticals
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
Discovery of small-molecule inhibitors selectively targeting the DNA-binding domain of the human androgen receptor.
University Of British Columbia
Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor.
Vancouver Prostate Centre (Vpc)
5'-Chloro-2,2'-dihydroxychalcone and related flavanoids as treatments for prostate cancer.
Kanazawa University
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs).
Marquette University
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
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Astrazeneca
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Oric Pharmaceuticals
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
The University Of Tokyo
High anticancer potency on tumor cells of dehydroabietylamine Schiff-base derivatives and a copper(II) complex.
Nanjing Forestry University
Exploring the tetrahydroisoquinoline thiohydantoin scaffold blockade the androgen receptor as potent anti-prostate cancer agents.
China Pharmaceutical University
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
Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.
Pfizer
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Pfizer
Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles.
Chinese Academy Of Sciences
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
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.
Drexel University College Of Medicine
An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy.
University Of Bonn
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
Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Janssen Research Foundation
Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine.
University Of Toronto