ArticleJournal of enzyme inhibition and medicinal chemistry2018
Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives.
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 16 papers.
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Who cites it
16 citing papers in PubMed.
- Estrogen Receptors and Enzymes Involved in Estrogen Synthesis as Breast Cancer Treatment Targets.International journal of molecular sciences · 2026Review
- TRPA1 Inhibition Effects by 3-Phenylcoumarin Derivatives.ACS medicinal chemistry letters · 2024Article
- Evaluation of Lippia scaberrima Sond. and Aspalathus linearis (Burm.f.) R. Dahlgren extracts on human CYP enzymes and gold nanoparticle synthesis: implications for drug metabolism and cytotoxicity.BMC complementary medicine and therapies · 2024Article
- Targeting the formation of estrogens for treatment of hormone dependent diseases-current status.Frontiers in pharmacology · 2023Review
- Western Diet Decreases Hepatic Drug Metabolism in Male LDLrJournal of nutrition and metabolism · 2023Article
- Natural source, bioactivity and synthesis of 3-Arylcoumarin derivatives.Journal of enzyme inhibition and medicinal chemistry · 2022Review
- In vitro metabolism of helenalin and its inhibitory effect on human cytochrome P450 activity.Archives of toxicology · 2022Article
- 3-Phenylcoumarins as a Privileged Scaffold in Medicinal Chemistry: The Landmarks of the Past Decade.Molecules (Basel, Switzerland) · 2021Review
- Coumarins as Tool Compounds to Aid the Discovery of Selective Function Modulators of Steroid Hormone Binding Proteins.Molecules (Basel, Switzerland) · 2021Review
- Substrate Selectivity of Coumarin Derivatives by Human CYP1 Enzymes: In Vitro Enzyme Kinetics and In Silico Modeling.ACS omega · 2021Article
- Coumarin-Based Profluorescent and Fluorescent Substrates for Determining Xenobiotic-Metabolizing Enzyme Activities In Vitro.International journal of molecular sciences · 2020Review
- A Perspective: Active Role of Lipids in Neurotransmitter Dynamics.Molecular neurobiology · 2020Review
- In Vitro Human Metabolism and Inhibition Potency of Verbascoside for CYP Enzymes.Molecules (Basel, Switzerland) · 2019Article
- A Practical Perspective: The Effect of Ligand Conformers on the Negative Image-Based Screening.International journal of molecular sciences · 2019Article
- Human cytochrome P450 enzymes 5-51 as targets of drugs and natural and environmental compounds: mechanisms, induction, and inhibition - toxic effects and benefits.Drug metabolism reviews · 2018Review
- Discovery of Retinoic Acid-Related Orphan Receptor γt Inverse Agonists via Docking and Negative Image-Based Screening.ACS omega · 2018Article
Corrections and comments
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Authors and funding
16 authors.
Funding
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Abstract
A comprehensive set of 3-phenylcoumarin analogues with polar substituents was synthesised for blocking oestradiol synthesis by 17-β-hydroxysteroid dehydrogenase 1 (HSD1) in the latter part of the sulphatase pathway. Five analogues produced ≥62% HSD1 inhibition at 5 µM and, furthermore, three of them produced ≥68% inhibition at 1 µM. A docking-based structure-activity relationship analysis was done to determine the molecular basis of the inhibition and the cross-reactivity of the analogues was tested against oestrogen receptor, aromatase, cytochrome P450 1A2, and monoamine oxidases. Most of the analogues are only modestly active with 17-β-hydroxysteroid dehydrogenase 2 - a requirement for lowering effective oestradiol levels in vivo. Moreover, the analysis led to the synthesis and discovery of 3-imidazolecoumarin as a potent aromatase inhibitor. In short, coumarin core can be tailored with specific ring and polar moiety substitutions to block either the sulphatase pathway or the aromatase pathway for treating breast cancer and endometriosis.
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