2-Hydroxy-2-methyl-N-(4-nitro-3-(trifluoromethyl)-phenyl)propanamide
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Anti-androgen 2-hydroxyflutamide modulates cadherin, catenin and androgen receptor phosphorylation in androgen-sensitive LNCaP and androgen-independent PC3 prostate cancer cell lines acting via PI3K/Akt and MAPK/ERK1/2 pathways. | Toxicology in vitro : an international journal published in association with BIBRA 20170401 |
Incorporation of a metabolizing system in biodetection assays for endocrine active substances. | ALTEX 20170101 |
TBECH, 1,2-dibromo-4-(1,2 dibromoethyl) cyclohexane, alters androgen receptor regulation in response to mutations associated with prostate cancer. | Toxicology and applied pharmacology 20160915 |
Development and pre-validation of an in vitro transactivation assay for detection of (anti)androgenic potential compounds using 22Rv1/MMTV cells. | Reproductive toxicology (Elmsford, N.Y.) 20160401 |
Effects of primary metabolites of organophosphate flame retardants on transcriptional activity via human nuclear receptors. | Toxicology letters 20160314 |
Hydroxyflutamide affects connexin 43 via the activation of PI3K/Akt-dependent pathway but has no effect on the crosstalk between PI3K/Akt and ERK1/2 pathways at the Raf-1 kinase level in primary rat Sertoli cells. | Toxicology in vitro : an international journal published in association with BIBRA 20160301 |
The ability of the YAS and AR CALUX assays to detect the additive effects of anti-androgenic fungicide mixtures. | Toxicology letters 20160122 |
Low dose evaluation of the antiandrogen flutamide following a Mode of Action approach. | Toxicology and applied pharmacology 20151215 |
The brominated flame retardants TBP-AE and TBP-DBPE antagonize the chicken androgen receptor and act as potential endocrine disrupters in chicken LMH cells. | Toxicology in vitro : an international journal published in association with BIBRA 20151201 |
Identification of a group of brominated flame retardants as novel androgen receptor antagonists and potential neuronal and endocrine disrupters. | Environment international 20150101 |
Metabolomics-on-a-chip of hepatotoxicity induced by anticancer drug flutamide and Its active metabolite hydroxyflutamide using HepG2/C3a microfluidic biochips. | Toxicological sciences : an official journal of the Society of Toxicology 20130301 |
Ligand-independent androgen receptor antagonism caused by the newly developed pesticide pyrifluquinazon (PFQ). | Reproductive toxicology (Elmsford, N.Y.) 20130101 |
Administration of flutamide alters sperm ultrastructure, sperm plasma membrane integrity and its stability, and sperm mitochondrial oxidative capability in the boar: in vivo and in vitro approach. | Reproduction in domestic animals = Zuchthygiene 20120801 |
Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators. | Journal of medicinal chemistry 20120726 |
Does 2-hydroxyflutamide inhibit apoptosis in porcine granulosa cells? - An in vitro study. | The Journal of reproduction and development 20120101 |
Androgen receptor coregulators NOCR1, TIF2, and ARA70 may account for the hydroxyflutamide insensitivity of prostate cancer cells. | Irish journal of medical science 20111201 |
A novel steroidal antiandrogen targeting wild type and mutant androgen receptors. | Biochemical pharmacology 20111201 |
Characterization of steroid hormone receptor activities in 100 hydroxylated polychlorinated biphenyls, including congeners identified in humans. | Toxicology 20111118 |
Development of 3-substituted-androsterone derivatives as potent inhibitors of 17β-hydroxysteroid dehydrogenase type 3. | Bioorganic & medicinal chemistry 20110801 |
Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets. | Journal of medicinal chemistry 20110609 |
Androgen receptors in the posterior bed nucleus of the stria terminalis increase neuropeptide expression and the stress-induced activation of the paraventricular nucleus of the hypothalamus. | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 20110601 |
Differential effects of a complex organochlorine mixture on the proliferation of breast cancer cell lines. | Environmental research 20110401 |
Hydroxyflutamide enhances cellular sensitivity to 5-fluorouracil by suppressing thymidylate synthase expression in bicalutamide-resistant human prostate cancer cells. | International journal of oncology 20110301 |
QSAR models for anti-androgenic effect--a preliminary study. | SAR and QSAR in environmental research 20110301 |
Production of human metabolites of the anti-cancer drug flutamide via biotransformation in Cunninghamella species. | Biotechnology letters 20110201 |
Modulation of androgen receptor signaling in hormonal therapy-resistant prostate cancer cell lines. | PloS one 20110101 |
The medial preoptic nucleus integrates the central influences of testosterone on the paraventricular nucleus of the hypothalamus and its extended circuitries. | The Journal of neuroscience : the official journal of the Society for Neuroscience 20100901 |
Cell viability and PSA secretion assays in LNCaP cells: a tiered in vitro approach to screen chemicals with a prostate-mediated effect on male reproduction within the ReProTect project. | Reproductive toxicology (Elmsford, N.Y.) 20100801 |
Determination of 2-hydroxyflutamide in human plasma by liquid chromatography-tandem mass spectrometry (LC-MS/MS): application to a bioequivalence study on Chinese volunteers. | Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20100601 |
A mouse model of androgenetic alopecia. | Endocrinology 20100501 |
Is the 'comb over' dying? A mouse model for male pattern baldness (androgenic alopecia). | Endocrinology 20100501 |
Systematic structure-function analysis of androgen receptor Leu701 mutants explains the properties of the prostate cancer mutant L701H. | The Journal of biological chemistry 20100212 |
Potent and selective steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 7, an enzyme that catalyzes the reduction of the key hormones estrone and dihydrotestosterone. | Journal of medicinal chemistry 20091210 |
Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. | Journal of medicinal chemistry 20091126 |
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. | Journal of natural products 20091101 |
Design and synthesis of androgen receptor antagonists with bulky side chains for overcoming antiandrogen resistance. | Journal of medicinal chemistry 20090910 |
Nuclear hormone receptor activity of polybrominated diphenyl ethers and their hydroxylated and methoxylated metabolites in transactivation assays using Chinese hamster ovary cells. | Environmental health perspectives 20090801 |
Suppression of mutant androgen receptors by flutamide. | International journal of urology : official journal of the Japanese Urological Association 20090501 |
Functional AR signaling is evident in an in vitro mouse follicle culture bioassay that encompasses most stages of folliculogenesis. | Biology of reproduction 20090401 |
Steroidal lactones as inhibitors of 17beta-hydroxysteroid dehydrogenase type 5: chemical synthesis, enzyme inhibitory activity, and assessment of estrogenic and androgenic activities. | European journal of medicinal chemistry 20090201 |
Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring. | Bioorganic & medicinal chemistry 20080901 |
Computationally identified novel diphenyl- and phenylpyridine androgen receptor antagonist structures. | Journal of chemical information and modeling 20080901 |
Nandrolone decreases mu opioid receptor expression in SH-SY5Y human neuroblastoma cells. | Neuroreport 20080716 |
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. | Bioorganic & medicinal chemistry 20080715 |
A new prostate cancer therapeutic approach: combination of androgen ablation with COX-2 inhibitor. | International journal of cancer 20080701 |
Screening of 397 chemicals and development of a quantitative structure--activity relationship model for androgen receptor antagonism. | Chemical research in toxicology 20080401 |
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists. | Bioorganic & medicinal chemistry letters 20080315 |
1,1-dichloro-2,2-bis(p-chlorophenyl)ethylene (p,p'-DDE) disrupts the estrogen-androgen balance regulating the growth of hormone-dependent breast cancer cells. | Breast cancer research : BCR 20080101 |
Testosterone directly induces progesterone production and interacts with physiological concentrations of LH to increase granulosa cell progesterone production in laying hens (Gallus domesticus). | Animal reproduction science 20071101 |
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. | Bioorganic & medicinal chemistry letters 20071015 |
PRMT2, a member of the protein arginine methyltransferase family, is a coactivator of the androgen receptor. | The Journal of steroid biochemistry and molecular biology 20071001 |
Transport, metabolism, and hepatotoxicity of flutamide, drug-drug interaction with acetaminophen involving phase I and phase II metabolites. | Chemical research in toxicology 20071001 |
Effects of steroidal and non-steroidal antiandrogens on wild-type and mutant androgen receptors. | The Prostate 20070601 |
Dihydrotestosterone inhibits tumor necrosis factor alpha induced interleukin-1alpha mRNA expression in rheumatoid fibroblast-like synovial cells. | Biological & pharmaceutical bulletin 20070601 |
Testosterone inhibits matrix metalloproteinase-1 production in human endometrial stromal cells in vitro. | Reproduction (Cambridge, England) 20070601 |
Non-steroidal antiandrogens act as AF-1 agonists under conditions of high androgen-receptor expression. | The Prostate 20070501 |
Chemical synthesis and biological activities of 16alpha-derivatives of 5alpha-androstane-3alpha,17beta-diol as antiandrogens. | Bioorganic & medicinal chemistry 20070415 |
Synthesis and biological evaluation of [18F]bicalutamide, 4-[76Br]bromobicalutamide, and 4-[76Br]bromo-thiobicalutamide as non-steroidal androgens for prostate cancer imaging. | Journal of medicinal chemistry 20070308 |
Ligand-specific dynamics of the androgen receptor at its response element in living cells. | Molecular and cellular biology 20070301 |
The androgen receptor T877A mutant recruits LXXLL and FXXLF peptides differently than wild-type androgen receptor in a time-resolved fluorescence resonance energy transfer assay. | Biochemistry 20070123 |
Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships. | Bioorganic & medicinal chemistry 20070101 |
Regulation of A Disintegrin And Metalloproteinase with ThromboSpondin repeats-1 expression in human endometrial stromal cells by gonadal steroids involves progestins, androgens, and estrogens. | The Journal of clinical endocrinology and metabolism 20061201 |
Prediction of estrogen receptor agonists and characterization of associated molecular descriptors by statistical learning methods. | Journal of molecular graphics & modelling 20061101 |
Anti-progestogenic effect of flutamide on uterine expression of calbindin-D9k mRNA and protein in immature mice. | Reproductive toxicology (Elmsford, N.Y.) 20061101 |
Chiral dimethylamine flutamide derivatives--modeling, synthesis, androgen receptor affinities and carbon-11 labeling. | Nuclear medicine and biology 20060801 |
Synthesis and biological evaluation of a nonsteroidal bromine-76-labeled androgen receptor ligand 3-[76Br]bromo-hydroxyflutamide. | Nuclear medicine and biology 20060801 |
Flutamide metabolism in four different species in vitro and identification of flutamide metabolites in human patient urine by high performance liquid chromatography/tandem mass spectrometry. | Drug metabolism and disposition: the biological fate of chemicals 20060601 |
Androgen effects on hippocampal CA1 spine synapse numbers are retained in Tfm male rats with defective androgen receptors. | Endocrinology 20060501 |
Microsphere-based protease assays and screening application for lethal factor and factor Xa. | Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501 |
Co-activator and co-repressor interplay on the human androgen receptor. | Andrologia 20051201 |
Prostate cancer PET bioprobes: synthesis of [18F]-radiolabeled hydroxyflutamide derivatives. | Bioorganic & medicinal chemistry 20051115 |
Androgens augment the mitogenic effects of oocyte-secreted factors and growth differentiation factor 9 on porcine granulosa cells. | Biology of reproduction 20051001 |
Antiandrogens prevent stable DNA-binding of the androgen receptor. | Journal of cell science 20050915 |
The structural basis of androgen receptor activation: intramolecular and intermolecular amino-carboxy interactions. | Proceedings of the National Academy of Sciences of the United States of America 20050712 |
5alpha-dihydrotestosterone inhibits 1alpha,25-dihydroxyvitamin D3-induced expression of CYP24 in human prostate cancer cells. | The Prostate 20050515 |
Castration reduces platelet thromboxane A2 receptor density and aggregability. | QJM : monthly journal of the Association of Physicians 20050501 |
Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. | Bioorganic & medicinal chemistry letters 20050117 |
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. | Bioorganic & medicinal chemistry letters 20050117 |
Dose-dependent transitions in mechanisms of toxicity: case studies. | Toxicology and applied pharmacology 20041215 |
Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia. | Endocrinology 20041201 |
The effects of the reported active metabolite of methoxychlor, 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane, on testosterone formation by cultured Leydig cells from young adult rats. | Reproductive toxicology (Elmsford, N.Y.) 20041101 |
Androgen receptor is targeted to distinct subcellular compartments in response to different therapeutic antiandrogens. | Clinical cancer research : an official journal of the American Association for Cancer Research 20041101 |
Functional domain and motif analyses of androgen receptor coregulator ARA70 and its differential expression in prostate cancer. | The Journal of biological chemistry 20040806 |
Interactions between androgen and growth factors in granulosa cell subtypes of porcine antral follicles. | Biology of reproduction 20040701 |
Differential effect of small ubiquitin-like modifier (SUMO)-ylation of the androgen receptor in the control of cooperativity on selective versus canonical response elements. | Molecular endocrinology (Baltimore, Md.) 20040601 |
Evidence that inhibited prostatic epithelial bud formation in 2,3,7,8-tetrachlorodibenzo-p-dioxin-exposed C57BL/6J fetal mice is not due to interruption of androgen signaling in the urogenital sinus. | Toxicological sciences : an official journal of the Society of Toxicology 20040601 |
Androgen receptor blockade in the MPOA or VMN: effects on male sociosexual behaviors. | Physiology & behavior 20040601 |
Effect of organochlorine pesticides on human androgen receptor activation in vitro. | Toxicology and applied pharmacology 20040415 |
[Examination of the change in plasma concentration of OH-flutamide in low-dose flutamide (250 mg/day) monotherapy for prostate cancer patients]. | Gan to kagaku ryoho. Cancer & chemotherapy 20040301 |
Ectopic expression of the amino-terminal peptide of androgen receptor leads to androgen receptor dysfunction and inhibition of androgen receptor-mediated prostate cancer growth. | Molecular and cellular endocrinology 20040212 |
Androgen inhibition of MAP kinase pathway and Elk-1 activation in proliferating osteoblasts. | Journal of molecular endocrinology 20040201 |
Screening of some anti-androgenic endocrine disruptors using a recombinant cell-based in vitro bioassay. | The Journal of steroid biochemistry and molecular biology 20040201 |
Proteasome inhibitors and their combination with antiandrogens: effects on apoptosis, cellular proliferation and viability of prostatic adenocarcinoma cell cultures. | Prostate cancer and prostatic diseases 20040101 |
Potential action of androstenedione on the proliferation and apoptosis of stromal endometrial cells. | Reproductive biology and endocrinology : RB&E 20040101 |
Androgen dependent regulation of bacillus Calmette-Guerin induced interleukin-6 expression in human transitional carcinoma cell lines. | The Journal of urology 20031101 |
Modulation of androgen receptor transactivation by gelsolin: a newly identified androgen receptor coregulator. | Cancer research 20030815 |
UV filters with antagonistic action at androgen receptors in the MDA-kb2 cell transcriptional-activation assay. | Toxicological sciences : an official journal of the Society of Toxicology 20030701 |
Inhibition of fatty acid synthase expression by 1alpha,25-dihydroxyvitamin D3 in prostate cancer cells. | The Journal of steroid biochemistry and molecular biology 20030501 |
Effects of hydroxyflutamide in the medial preoptic area or lateral septum on reproductive behaviors in male rats. | Brain research bulletin 20021130 |
Activation of mitogen-activated protein kinase pathway by the antiandrogen hydroxyflutamide in androgen receptor-negative prostate cancer cells. | Cancer research 20021101 |
Nerve growth factor induces the re-expression of functional androgen receptors and p75(NGFR) in the androgen-insensitive prostate cancer cell line DU145. | European journal of endocrinology 20020901 |
[Sex-difference on flutamide metabolism in rat liver microsomal cytochrome P450 1A2]. | Yao xue xue bao = Acta pharmaceutica Sinica 20020801 |
Pure antiandrogens disrupt the recruitment of coactivator GRIP1 to colocalize with androgen receptor in nuclei. | FEBS letters 20020717 |
Acquisition of agonistic properties of nonsteroidal antiandrogens after treatment with oncostatin M in prostate cancer cells. | Clinical cancer research : an official journal of the American Association for Cancer Research 20020701 |
Stabilization of androgen receptor protein is induced by agonist, not by antagonists. | Biochemical and biophysical research communications 20020621 |
Androgens protect against apolipoprotein E4-induced cognitive deficits. | The Journal of neuroscience : the official journal of the Society for Neuroscience 20020615 |
Cytotoxicity of flutamide and 2-hydroxyflutamide and their effects on CYP1A2 mRNA in primary rat hepatocytes. | Acta pharmacologica Sinica 20020601 |
The amino terminus of the human AR is target for corepressor action and antihormone agonism. | Molecular endocrinology (Baltimore, Md.) 20020401 |
A novel cell line, MDA-kb2, that stably expresses an androgen- and glucocorticoid-responsive reporter for the detection of hormone receptor agonists and antagonists. | Toxicological sciences : an official journal of the Society of Toxicology 20020301 |
Development of two androgen receptor assays using adenoviral transduction of MMTV-luc reporter and/or hAR for endocrine screening. | Toxicological sciences : an official journal of the Society of Toxicology 20020301 |
Role of cadmium in the regulation of AR gene expression and activity. | Endocrinology 20020101 |
Use of the probasin promoter ARR2PB to express Bax in androgen receptor-positive prostate cancer cells. | Journal of the National Cancer Institute 20010905 |
Determination of 2-hydroxyflutamide in human plasma by high-performance liquid chromatography and its application to pharmacokinetic studies. | Journal of chromatography. B, Biomedical sciences and applications 20010805 |
The subnuclear three-dimensional image analysis of androgen receptor fused to green fluorescence protein. | The Journal of biological chemistry 20010727 |
Homology modeling using multiple molecular dynamics simulations and docking studies of the human androgen receptor ligand binding domain bound to testosterone and nonsteroidal ligands. | Journal of medicinal chemistry 20010524 |
Dexamethasone blocks antioestrogen- and oxidant-induced death of pituitary tumour cells. | The Journal of endocrinology 20010501 |
Testosterone inhibits osteoclast formation stimulated by parathyroid hormone through androgen receptor. | FEBS letters 20010223 |
Mutations at the boundary of the hinge and ligand binding domain of the androgen receptor confer increased transactivation function. | Molecular endocrinology (Baltimore, Md.) 20010101 |
Androgen-induced cell growth and c-myc expression in human non-transformed epithelial prostatic cells in primary culture. | Endocrine research 20010101 |
Regulation of GCDFP-15 expression in human mammary cancer cells. | International journal of molecular medicine 19990801 |
Rapid and sensitive reporter gene assays for detection of antiandrogenic and estrogenic effects of environmental chemicals. | Toxicology and applied pharmacology 19990301 |
Inhibition of androgen receptor-dependent transcriptional activity by DDT isomers and methoxychlor in HepG2 human hepatoma cells. | Toxicology and applied pharmacology 19980701 |
Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. | Biochemical pharmacology 19980501 |
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. | Journal of medicinal chemistry 19980212 |
Comparison of in vitro effects of the pure antiandrogens OH-flutamide, Casodex, and nilutamide on androgen-sensitive parameters. | Urology 19970401 |
Evaluation of chemicals with endocrine modulating activity in a yeast-based steroid hormone receptor gene transcription assay. | Toxicology and applied pharmacology 19970301 |
Non-steroidal L-245,976 acts as a classical antiandrogen in vitro. | The Journal of steroid biochemistry and molecular biology 19970101 |
The pharmacokinetics of flutamide and its major metabolites after a single oral dose and during chronic treatment. | European journal of clinical pharmacology 19880101 |