ArticleJournal of medicinal chemistry2015
Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 78 citations in OpenAlex.
- Discovery and development of steroidal enzyme inhibitors as anti-cancer drugs: state-of-the-art and future perspectives.Journal of enzyme inhibition and medicinal chemistry · 2025Review
- The anti-amoebic potential of carboxamide derivatives containing sulfonyl or sulfamoyl moieties against brain-eating Naegleria fowleri.Parasitology research · 2023Article
- 2-Methoxyestradiol-3,17-International journal of molecular sciences · 2023Article
- Description of Chemical Synthesis, Nuclear Magnetic Resonance Characterization and Biological Activity of Estrane-Based Inhibitors/Activators of Steroidogenesis.Molecules (Basel, Switzerland) · 2023Review
- Novel Anti-Acanthamoebic Activities of Irosustat and STX140 and Their Nanoformulations.Antibiotics (Basel, Switzerland) · 2023Article
- 2-Difluoromethoxy-Substituted Estratriene Sulfamates: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Steroid Sulfatase Inhibition.ChemMedChem · 2022Article
- Development of Sulfamoylated 4-(1-Phenyl-1Journal of medicinal chemistry · 2022Article
- Transition metal-catalysed A-ring C-H activations and C(spJournal of enzyme inhibition and medicinal chemistry · 2021Article
- Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.RSC medicinal chemistry · 2021Article
- Steroid Sulphatase and Its Inhibitors: Past, Present, and Future.Molecules (Basel, Switzerland) · 2021Review
- 2-Methoxyestradiol and its derivatives inhibit store-operated CaBiochimica et biophysica acta. Molecular cell research · 2021Article
- Article
- Recent progress in the development of steroid sulphatase inhibitors - examples of the novel and most promising compounds from the last decade.Journal of enzyme inhibition and medicinal chemistry · 2020Review
- Synthesis of Tamoxifen-Artemisinin and Estrogen-Artemisinin Hybrids Highly Potent Against Breast and Prostate Cancer.ChemMedChem · 2020Article
- Nonsteroidal sulfamate derivatives as new therapeutic approaches for Neurofibromatosis 2 (NF2).BMC pharmacology & toxicology · 2019Article
- Article
- Transient [3,3] Cope rearrangement of 3,3-dicyano-1,5-dienes: computational analysis and 2-step synthesis of arylcycloheptanes.Chemical science · 2018Article
- C-3- and C-4-Substituted Bicyclic Coumarin Sulfamates as Potent Steroid Sulfatase Inhibitors.ACS omega · 2018Article
- Virtual screening applications in short-chain dehydrogenase/reductase research.The Journal of steroid biochemistry and molecular biology · 2017Review
- Design, synthesis, and biological evaluation of new arylamide derivatives possessing sulfonate or sulfamate moieties as steroid sulfatase enzyme inhibitors.Bioorganic & medicinal chemistry · 2016Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
Abstract
In 1994, following work from this laboratory, it was reported that estrone-3-O-sulfamate irreversibly inhibits a new potential hormone-dependent cancer target steroid sulfatase (STS). Subsequent drug discovery projects were initiated to develop the core aryl O-sulfamate pharmacophore that, over some 20 years, have led to steroidal and nonsteroidal drugs in numerous preclinical and clinical trials, with promising results in oncology and women's health, including endometriosis. Drugs have been designed to inhibit STS, e.g., Irosustat, as innovative dual-targeting aromatase-steroid sulfatase inhibitors (DASIs) and as multitargeting agents for hormone-independent tumors, such as the steroidal STX140 and nonsteroidal counterparts, acting inter alia through microtubule disruption. The aryl sulfamate pharmacophore is highly versatile, operating via three distinct mechanisms of action, and imbues attractive pharmaceutical properties. This Perspective gives a personal view of the work leading both to the therapeutic concepts and these drugs, their current status, and how they might develop in the future.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.