ArticleJournal of enzyme inhibition and medicinal chemistry2022
Interaction of letrozole and its degradation products with aromatase: chemometric assessment of kinetics and structure-based binding validation.
Article in Journal of enzyme inhibition and medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 12 citations in OpenAlex.
- Molecular insights into Silodosin's anti-cancer effects: a promising repurposing strategy for breast cancer.Cell death discovery · 2026Article
- Article
- Comparative effects of streptozotocin, dehydroepiandrosterone and letrozole with high fat diet on ovarian injury induction and functional impairment.Scientific reports · 2025Article
- Pharmacophore-based virtual screening, molecular docking, and molecular dynamics investigation for the identification of novel, marine aromatase inhibitors.BMC chemistry · 2024Article
- Dual-responsive chondroitin sulfate self-assembling nanoparticles for combination therapy in metastatic cancer cells.International journal of pharmaceutics: X · 2024Article
- A comparative study of green solid contact ion selective electrodes for the potentiometric determination of Letrozole in dosage form and human plasma.Scientific reports · 2023Article
- Design of Novel Letrozole Analogues Targeting Aromatase for Breast Cancer: Molecular Docking, Molecular Dynamics, and Theoretical Studies on Gold Nanoparticles.Metabolites · 2023Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Letrozole is one of the most prescribed drugs for the treatment of breast cancer in post-menopausal women, and it is endowed with selective peripheral aromatase inhibitory activity. The efficacy of this drug is also a consequence of its long-lasting activity, likely due to its metabolic stability. The reactivity of cyano groups in the letrozole structure could, however, lead to chemical derivatives still endowed with residual biological activity. Herein, the chemical degradation process of the drug was studied by coupling multivariate curve resolution and spectrophotometric methodologies in order to assess a detailed kinetic profile. Three main derivatives were identified after drug exposure to different degradation conditions, consisting of acid-base and oxidative environments and stressing light. Molecular docking confirmed the capability of these compounds to accommodate into the active site of the enzyme, suggesting that the sustained inhibitory activity of letrozole may be at least in part attributed to the degradation compounds.
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Registered trials
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