ArticleJournal of enzyme inhibition and medicinal chemistry2023
Selenium-analogs based on natural sources as cancer-associated carbonic anhydrase isoforms IX and XII inhibitors.
Article in Journal of enzyme inhibition and medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed, 19 citations in OpenAlex.
- Natural Histidine Derivatives-From Basic Research to Potential Applications in Cosmetics and Nutricosmetics.Antioxidants (Basel, Switzerland) · 2026Review
- New Se-Compounds With Antileishmanial, Antitumor, and Carbonic Anhydrase Inhibitory Properties.Archiv der Pharmazie · 2025Article
- New Dimethoxyaryl-Sesquiterpene Derivatives with Cytotoxic Activity Against MCF-7 Breast Cancer Cells: From Synthesis to Topoisomerase I/II Inhibition and Cell Death Mechanism Studies.International journal of molecular sciences · 2025Article
- Exploration of Aromatic Hydrazides as Inhibitors of Human Carbonic Anhydrases.Archiv der Pharmazie · 2025Article
- Article
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
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Abstract
In the relentless search for new cancer treatments, organoselenium compounds, and carbonic anhydrase (CA) inhibitors have emerged as promising drug candidates. CA isoforms IX and XII are overexpressed in many types of cancer, and their inhibition is associated with potent antitumor/antimetastatic effects. Selenium-containing compounds, particularly selenols, have been shown to inhibit tumour-associated CA isoforms in the nanomolar range since the properties of the selenium atom favour binding to the active site of the enzyme. In this work, two series of selenoesters (1a-19a and 1b-19b), which gathered NSAIDs, carbo/heterocycles, and fragments from natural products, were evaluated against hCA I, II, IX, and XII. Indomethacin (17b) and flufenamic acid (19b) analogs exhibited selectivity for tumour-associated isoform IX in the low micromolar range. In summary, selenoesters that combine NSAIDs with fragments derived from natural sources have been developed as promising nonclassical inhibitors of the tumour-associated CA isoforms.
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