In vivo inhibition of estrone sulfatase activity and growth of nitrosomethylurea-induced mammary tumors by 667 COUMATE.

No abstract is available for this paper.

• Publication year

  2000

• Venue

  Cancer Research

• Publication date

  2000-07-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  PMID 10910045
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Recent advances in the development of steroid sulphatase inhibitors.

  1999cited by this paper
• Potent inhibition of steroid sulfatase activity by 3-O-sulfamate 17alpha-benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: combination of two substituents at positions C3 and c17alpha of estradiol.

  1999cited by this paper
• Pharmacology of Inhibitors of Estrogen Biosynthesis

  1999cited by this paper
• Development of potent non-estrogenic estrone sulfatase inhibitors.

  1998cited by this paper
• Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates.

  1996cited by this paper
• Aromatase inhibitors--where are we now?

  1996cited by this paper
• The development of steroid sulphatase inhibitors

  1996cited by this paper
• Synthesis and sulfatase inhibitory activities of non-steroidal estrone sulfatase inhibitors.

  1996cited by this paper
• In vivo activity of 4-methylcoumarin-7-O-sulfamate, a nonsteroidal, nonestrogenic steroid sulfatase inhibitor.

  1996cited by this paper
• Sulfamates of various estrogens are prodrugs with increased systemic and reduced hepatic estrogenicity at oral application.

  1995cited by this paper
• Inactivation of steroid sulfatase by an active site-directed inhibitor, estrone-3-O-sulfamate.

  1995cited by this paper
• In vivo inhibition of oestrone sulphatase and dehydroepiandrosterone sulphatase by oestrone‐3‐O‐sulphamate

  1995cited by this paper
• The hydrolysis of oestrone sulphate and dehydroepiandrosterone sulphate by human steroid sulphatase expressed in transfected COS-1 cells.

  1994cited by this paper
• Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential.

  1994cited by this paper
• Inhibition of estrone sulfatase activity by estrone-3-methylthiophosphonate: a potential therapeutic agent in breast cancer.

  1993cited by this paper
• Androstenedione and androst-5-ene-3 beta,17 beta-diol stimulate DMBA-induced rat mammary tumors--role of aromatase.

  1989cited by this paper
• Stimulation of cell proliferation and estrogenic response by adrenal C19-delta 5-steroids in the ZR-75-1 human breast cancer cell line.

  1986cited by this paper

• Steroid sulfatase: A systematic study on the isolation, single step purification, and identification of its new inhibitors

  2025cites this paper
• New Insights into the Plutella xylostella Detoxifying Enzymes: Sequence Evolution, Structural Similarity, Functional Diversity, and Application Prospects of Glucosinolate Sulfatases

  2023cites this paper
• Host modulation therapy for improving the osseointegration of dental implants under bone healing-suppressed conditions: a preclinical rodent-model experiment

  2023cites this paper
• University of Birmingham Steroid sulphatase and its inhibitors

  2021cites this paper
• Steroid Sulphatase and Its Inhibitors: Past, Present, and Future

  2021cites this paper
• Sulfamates in drug design and discovery: Pre-clinical and clinical investigations.

  2019cites this paper
• An efficient, mild and metal free l-proline catalyzed construction of fused pyrimidines under microwave conditions in water

  2019cites this paper
• Brain Gene Expression in a Novel Mouse Model of Postpartum Mood Disorder

  2019cites this paper
• Metal-Free Construction of Fused Pyrimidines via Consecutive C–C and C–N Bond Formation in Water

  2018cites this paper
• Steroid sulfatase inhibition success and limitation in breast cancer clinical assays: An underlying mechanism.

  2018cites this paper
• Novel p-carborane-containing multitarget anticancer agents inspired by the metabolism of 17β-estradiol.

  2017cites this paper
• Chiral phosphine-mediated intramolecular [3 + 2] annulation: enhanced enantioselectivity by achiral Brønsted acid† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c7sc00952f Click here for additional data file.

  2017cites this paper
• IPET study: an FLT-PET window study to assess the activity of the steroid sulfatase inhibitor irosustat in early breast cancer

  2017cites this paper
• Estrogen-Metabolizing Enzymes in Systemic and Local Liver Injuries: A Case Study of Disease–Drug Interaction

  2017cites this paper
• Design and synthesis of p-carborane-containing sulfamates as multitarget anti-breast cancer agents.

  2017cites this paper
• Inflammatory regulation of steroid sulfatase: A novel mechanism to control estrogen homeostasis and inflammation in chronic liver disease.

  2016cites this paper
• The Role of Steroid Sulfatase as a Prognostic Factor in Patients with Endometrial Cancer

  2016cites this paper
• A pharmacological mouse model suggests a novel risk pathway for postpartum psychosis

  2016cites this paper
• Contribution of Estrone Sulfate to Cell Proliferation in Aromatase Inhibitor (AI) -Resistant, Hormone Receptor-Positive Breast Cancer

  2016cites this paper
• Eco-friendly grinding synthesis of a double-layered nanomaterial and the correlation between its basicity, calcination and catalytic activity in the green synthesis of novel fused pyrimidines

  2016cites this paper
• Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors.

  2015cites this paper
• Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.

  2015cites this paper
• Synthesis and steroid sulfatase inhibitory activities of N-alkanoyl tyramine phosphates and thiophosphates†

  2015cites this paper
• Synthesis and Cytotoxic Evaluation of Pyran, Dihydropyridine and Thiophene Derivatives of 3-Acetylcoumarin.

  2015cites this paper
• Characterization and Regulation of Steroid Sulfatase in the Human MG-63 Pre-osteoblastic Cell Line

  2015cites this paper
• Estrogen O-sulfamates and their analogues: Clinical steroid sulfatase inhibitors with broad potential.

  2015cites this paper
• The Regulation of Steroid Action by Sulfation and Desulfation

  2015cites this paper
• Population Pharmacokinetic Modelling of Irosustat in Postmenopausal Women with Oestrogen-Receptor Positive Breast Cancer Incorporating Non-Linear Red Blood Cell Uptake

  2014cites this paper
• Synthesis and biological evaluation of 4-(1,2,3-triazol-1-yl)coumarin derivatives as potential antitumor agents.

  2014cites this paper
• Synthesis, structure-activity relationship of iodinated-4-aryloxymethyl-coumarins as potential anti-cancer and anti-mycobacterial agents.

  2014cites this paper
• Inhibition of dehydroepiandosterone sulfate action in androgen-sensitive tissues by EM-1913, an inhibitor of steroid sulfatase.

  2013cites this paper
• Steroid sulfatase inhibitors: promising new therapy for breast cancer.

  2013cites this paper
• In vitro metabolism and drug-drug interaction potential of irosustat, a steroidal sulfatase inhibitor

  2013cites this paper
• Steroid sulfatase inhibitors for estrogen- and androgen-dependent cancers.

  2012influential citation
• In Vitro Evaluation of the Interaction Potential of Irosustat with Drug-Metabolizing Enzymes

  2012cites this paper
• Impact of cows’ milk estrogen on cancer risk

  2012cites this paper
• Estudio farmacocinético preclínico de un inhibidor de la sulfatasa esteroidal

  2012cites this paper
• Multiple binding modes of inhibitors to carbonic anhydrases: how to design specific drugs targeting 15 different isoforms?

  2012cites this paper
• Steroid sulfatase inhibitors: promising new tools for breast cancer therapy?

  2011cites this paper
• Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer

  2011cites this paper
• Steroid sulfatase inhibitors: a review covering the promising 2000-2010 decade.

  2011cites this paper
• In Vitro Metabolism of Irosustat, a Novel Steroid Sulfatase Inhibitor: Interspecies Comparison, Metabolite Identification, and Metabolic Enzyme Identification

  2011cites this paper
• In Vitro Metabolism of Irosustat, a Novel Steroid Sulphatase Inhibitor: Inter-Species Comparison, Metabolite Identification and Metabolic Enzyme Identification

  2011cites this paper
• Recent advancement in nonsteroidal aromatase inhibitors for treatment of estrogen-dependent breast cancer.

  2010cites this paper
• Bicyclic Derivatives of the Potent Dual Aromatase–Steroid Sulfatase Inhibitor 2‐Bromo‐4‐{[(4‐cyanophenyl)(4H‐1,2,4‐triazol‐4‐yl)amino]methyl}phenylsulfamate: Synthesis, SAR, Crystal Structure, and in vitro and in vivo Activities

  2010cites this paper
• Shu-Gan-Liang-Xue Decoction, a Chinese herbal formula, down-regulates the expression of steroid sulfatase genes in human breast carcinoma MCF-7 cells.

  2010cites this paper
• Oestrogen-synthesising enzymes and breast cancer.

  2009cites this paper
• Shikonin, an ingredient of Lithospermum erythrorhizon, down-regulates the expression of steroid sulfatase genes in breast cancer cells.

  2009cites this paper
• Anticancer steroid sulfatase inhibitors: synthesis of a potent fluorinated second-generation agent, in vitro and in vivo activities, molecular modeling, and protein crystallography

  2008cites this paper
• Recent developments of steroid sulfatase inhibitors as anti-cancer agents.

  2008cites this paper
• 17β‐hydroxysteroid dehydrogenase Type 1, and not Type 12, is a target for endocrine therapy of hormone‐dependent breast cancer

  2008cites this paper
• A review of coumarin derivatives in pharmacotherapy of breast cancer.

  2008cites this paper
• The use of steroid sulfatase inhibitors as a novel therapeutic strategy against hormone-dependent endometrial cancer.

  2008cites this paper
• Efficacy of three potent steroid sulfatase inhibitors: pre-clinical investigations for their use in the treatment of hormone-dependent breast cancer

  2008cites this paper
• Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity.

  2008cites this paper
• Oestrogen producing enzymes and mammary carcinogenesis: a review

  2008cites this paper
• Steroid metabolism in breast cancer.

  2008cites this paper
• Studying plant-derived coumarins for their pharmacological and therapeutic properties as potential anticancer drugs

  2007cites this paper
• Characterization of Steroid Sulfatase in Human and Mouse Tissues and in the Mouse MC3T3-E1 Pre-Osteoblastic Cell Line

  2007cites this paper
• A novel dual-target steroid sulfatase inhibitor and antiestrogen: SR 16157, a promising agent for the therapy of breast cancer

  2007cites this paper
• Steroid sulfatase: a new target for the endocrine therapy of breast cancer.

  2007cites this paper
• A novel steroidal selective steroid sulfatase inhibitor KW-2581 inhibits sulfated-estrogen dependent growth of breast cancer cells in vitro and in animal models

  2007cites this paper
• New analogs of D-homoequilenine with substituents in the D ring

  2006cites this paper
• The regulation and inhibition of 17beta-hydroxysteroid dehydrogenase in breast cancer.

  2006cites this paper
• In vivo Efficacy of STX213, A Second-Generation Steroid Sulfatase Inhibitor, for Hormone-Dependent Breast Cancer Therapy

  2006cites this paper
• Phase I Study of STX 64 (667 Coumate) in Breast Cancer Patients: The First Study of a Steroid Sulfatase Inhibitor

  2006cites this paper
• Steroid sulfatase inhibitors

  2005cites this paper
• The effects of 2-methoxyoestrogen sulphamates on the in vitro and in vivo proliferation of breast cancer cells.

  2005cites this paper
• Steroid sulfatase: molecular biology, regulation, and inhibition.

  2005cites this paper
• A letrozole-based dual aromatase-sulphatase inhibitor with in vivo activity.

  2005cites this paper
• 6-[2-(adamantylidene)-hydroxybenzoxazole]-O-sulfamate, a steroid sulfatase inhibitor for the treatment of androgen- and estrogen-dependent diseases.

  2004cites this paper
• Pharmacokinetics of the nonsteroidal steroid sulphatase inhibitor 667 COUMATE and its sequestration into red blood cells in rats

  2004influential citation
• Development of novel steroid sulfatase inhibitors; II. TZS-8478 potently inhibits the growth of breast tumors in postmenopausal breast cancer model rats.

  2004cites this paper
• Synthesis, in vitro and in vivo activity of benzophenone-based inhibitors of steroid sulfatase.

  2004cites this paper
• The role of steroid sulphatase in regulating the oestrogenicity of oestrogen sulphamates.

  2004cites this paper
• Molecular structures of 17αβ-acetoxy-3-methoxy-6-oxa-D-homo-8-isoestra-1,3,5(10)-triene and its 4-methyl derivative

  2004cites this paper
• Role of steroid sulfatase in local formation of estrogen in post-menopausal breast cancer patients.

  2003cites this paper
• Regulation of Steroid Sulfatase in Human Breast Cancer Cells and Screening of Human Tissues for Steroid Sulfatase Status

  2003cites this paper
• Steroid sulfatase inhibitors

  2003cites this paper
• Development of a sensitive high-performance liquid chromatography method for the detection of 667 COUMATE in vivo.

  2003cites this paper
• Development of novel steroid sulfatase inhibitors. I. Synthesis and biological evaluation of biphenyl-4-O-sulfamates.

  2003cites this paper
• Steroid sulphatase inhibitors for breast cancer therapy.

  2003cites this paper
• Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2-methoxyoestradiol-bis-sulphamate.

  2003cites this paper
• In vitro and in vivo models for the evaluation of new inhibitors of human steroid sulfatase, devoid of residual estrogenic activity.

  2003cites this paper
• Design, synthesis and biochemical evaluation of AC ring mimics as novel inhibitors of the enzyme estrone sulfatase (ES).

  2002cites this paper
• [NMR spectroscopy for studying structure and intramolecular dynamics of modified analogs of steroid hormones].

  2002cites this paper
• The Synthesis and Properties of B-Nor-8-Isoanalogues of Steroid Estrogens

  2002cites this paper
• Nonsteroidal compounds designed to mimic potent steroid sulfatase inhibitors.

  2002cites this paper
• A multidetachable sulfamate linker successfully used in a solid-phase strategy to generate libraries of sulfamate and phenol derivatives.

  2002cites this paper
• Synthesis and biochemical evaluation of novel and potent inhibitors of the enzyme oestrone sulphatase (ES).

  2002cites this paper
• An NMR Study of the Spatial Structure and Intramolecular Dynamics of Modified Analogues of Steroid Hormones

  2002cites this paper
• Effect of tibolone (Org OD14) and its metabolites on aromatase and estrone sulfatase activity in human breast adipose stromal cells and in MCF-7 and T47D breast cancer cells.

  2002cites this paper
• Characterization of iodothyronine sulfatase activities in human and rat liver and placenta.

  2002cites this paper
• 2-Substituted 4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.

  2002cites this paper
• Differing Effects of Endocrine-Disrupting Chemicals on Basal and FSH-Stimulated Progesterone Production in Rat Granulosa-Luteal Cells

  2001cites this paper
• The selective estrogen enzyme modulator (SEEM) in breast cancer.

  2001cites this paper
• Inhibitors of steroidogenesis as agents for the treatment of hormone-dependent cancers

  2001cites this paper
• Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanism.

  2001cites this paper
• Potent active site-directed inhibition of steroid sulphatase by tricyclic coumarin-based sulphamates.

  2000cites this paper
• Inhibition of steroid sulphatase activity by tricyclic coumarin sulphamates.

  2000cites this paper