ArticleJournal of enzyme inhibition and medicinal chemistry2018
Synthesis and structure-activity relationships of 2- and/or 4-halogenated 13β- and 13α-estrone derivatives as enzyme inhibitors of estrogen biosynthesis.
Article in Journal of enzyme inhibition and medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 32 citations in OpenAlex.
- Biological and computer-aided evaluation of 3-methoxy-13α-estrone-16α-diphenylphosphine oxide as a new antiestrogenic agent.Scientific reports · 2025Article
- 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
- Synthesis and Antiproliferative Activity of Steroidal Diaryl Ethers.Molecules (Basel, Switzerland) · 2023Article
- Synthesis and evaluation of AKR1C inhibitory properties of A-ring halogenated oestrone derivatives.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Synthesis and evaluation of anticancer activities of 2- or 4-substituted 3-(Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Transition metal-catalysed A-ring C-H activations and C(spJournal of enzyme inhibition and medicinal chemistry · 2021Article
- Microwave-assisted Phospha-Michael addition reactions in the 13α-oestrone series andJournal of enzyme inhibition and medicinal chemistry · 2021Article
- Data-Driven Ensemble Docking to Map Molecular Interactions of Steroid Analogs with Hepatic Organic Anion Transporting Polypeptides.Journal of chemical information and modeling · 2021Article
- 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, Biological Evaluation and Docking Studies of 13-Epimeric 10-fluoro- and 10-Chloroestra-1,4-dien-3-ones as Potential Aromatase Inhibitors.Molecules (Basel, Switzerland) · 2019Article
- Synthesis of Novel C-2- or C-15-Labeled BODIPY-Estrone Conjugates.Molecules (Basel, Switzerland) · 2018Article
- Pd-Catalyzed microwave-assisted synthesis of phosphonated 13α-estrones as potential OATP2B1, 17β-HSD1 and/or STS inhibitors.Beilstein journal of organic chemistry · 2018Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ring A halogenated 13α-, 13β-, and 17-deoxy-13α-estrone derivatives were synthesised with N-halosuccinimides as electrophile triggers. Substitutions occurred at positions C-2 and/or C-4. The potential inhibitory action of the halogenated estrones on human aromatase, steroid sulfatase, or 17β-hydroxysteroid dehydrogenase 1 activity was investigated via in vitro radiosubstrate incubation. Potent submicromolar or low micromolar inhibitors were identified with occasional dual or multiple inhibitory properties. Valuable structure-activity relationships were established from the comparison of the inhibitory data obtained. Kinetic experiments performed with selected compounds revealed competitive reversible inhibition mechanisms against 17β-hydroxysteroid dehydrogenase 1 and competitive irreversible manner in the inhibition of the steroid sulfatase enzyme.
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