ArticleEuropean journal of medicinal chemistry2017
Structural basis for selective inhibition of Cyclooxygenase-1 (COX-1) by diarylisoxazoles mofezolac and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6).
Article in European journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 88 citations in OpenAlex.
- Analysis of Two New Flavonoid Glycosides FromAnalytical science advances · 2026Article
- Piperazine-Thiourea Hybrids as Novel Antiplatelet Agents Targeting COX-1: Synthesis,ACS omega · 2026Article
- Enzyme-Targeted Antiproliferative Effects of Novel Indole-Acrylamide Xenobiotics Acting on Cyclooxygenase Pathways.Journal of xenobiotics · 2026Article
- Design, Synthesis, and In Vitro Enzymatic Evaluation of Novel Flavone Derivatives as Dual COX-2/5-LOX Inhibitors Supported by Molecular Docking and ADMET Analysis.Current issues in molecular biology · 2026Article
- Advances in isoxazole chemistry and their role in drug discovery.RSC advances · 2025Review
- Evaluation of In Vitro and In Vivo Pharmacological Activity ofFood science & nutrition · 2025Article
- Comparative metabolic study of the chloroform fraction of threeJournal of enzyme inhibition and medicinal chemistry · 2024Article
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- Investigation of the Anti-Inflammatory Properties of Bioactive Compounds fromMolecules (Basel, Switzerland) · 2024Article
- Unveiling the pharmacological potential ofFood science & nutrition · 2024Article
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- Learning from Nature: From a Marine Natural Product to Synthetic Cyclooxygenase-1 Inhibitors by Automated De Novo Design.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2021Article
- Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.ACS medicinal chemistry letters · 2021Article
- Synthesis, Inhibitory Activity, andACS medicinal chemistry letters · 2021Article
- Three-dimensional structure of human cyclooxygenase (hCOX)-1.Scientific reports · 2021Article
- Targeted Detection of Cyclooxygenase-1 in Ovarian Cancer.ACS medicinal chemistry letters · 2020Article
- Structural and Chemical Biology of the Interaction of Cyclooxygenase with Substrates and Non-Steroidal Anti-Inflammatory Drugs.Chemical reviews · 2020Review
- Spiroindolone analogues bearing benzofuran moiety as a selective cyclooxygenase COX-1 with TNF-α and IL-6 inhibitors.Saudi journal of biological sciences · 2020Article
- Article
- An Activity-Based Sensing Approach for the Detection of Cyclooxygenase-2 in Live Cells.Angewandte Chemie (International ed. in English) · 2020Article
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
Abstract
The diarylisoxazole molecular scaffold is found in several NSAIDs, especially those with high selectivity for COX-1. Here, we have determined the structural basis for COX-1 binding to two diarylisoxazoles: mofezolac, which is polar and ionizable, and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6) that has very low polarity. X-ray analysis of the crystal structures of COX-1 bound to mofezolac and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole allowed the identification of specific binding determinants within the enzyme active site, relevant to generate structure/activity relationships for diarylisoxazole NSAIDs.
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