ArticleBMC chemistry2023
Design, synthesis, molecular docking studies and biological evaluation of thiazole carboxamide derivatives as COX inhibitors.
Article in BMC chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers, 1 of them a synthesis that pooled it.
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Who cites it
15 citing papers in PubMed, 1 synthesis or guideline pooled it, 28 citations in OpenAlex.
- The antidepressive mechanism of Longya Lilium combined with Fluoxetine in mice with depression-like behaviors.NPJ systems biology and applications · 2024Pooled it
- Quinazolinone-diarylpyrazole hybrids as dual EGFR/COX-2 inhibitors: antiproliferative, mechanistic, andRSC advances · 2026Article
- In Vitro and In Silico Insights into the Antiproliferative Activity of Sesquiterpenes fromInternational journal of molecular sciences · 2026Article
- Recent advances in thiazole-based derivatives targeting diverse anti-inflammatory pathways.RSC advances · 2026Review
- Recent Advances in the Therapeutic Prospective of Heterocyclic Derivatives as COX-2 Inhibitors (2019-Present).Mini reviews in medicinal chemistry · 2026Review
- Trifluoromethyl-pyrazole-carboxamides as COX inhibitors: synthesis, microed structural analysis, computational profiling, and biological evaluation.BMC chemistry · 2025Article
- Synthesis, Anti-Inflammatory, and Molecular Docking Studies of New Heterocyclic Derivatives Comprising Pyrazole, Pyridine, and/or Pyran Moieties.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Thiazole-carboxamide derivatives as potent antioxidant agents with drug-like properties: In vitro, molecular docking, and DFT studies.PloS one · 2025Article
- Review
- Explainable artificial intelligence-assisted virtual screening and bioinformatics approaches for effective bioactivity prediction of phenolic cyclooxygenase-2 (COX-2) inhibitors using PubChem molecular fingerprints.Molecular diversity · 2024Article
- Assessing the Effects of Thiazole-Carboxamide Derivatives on the Biophysical Properties of AMPA Receptor Complexes as a Potential Neuroprotective Agent.Molecules (Basel, Switzerland) · 2024Article
- Synthesis, Characterization, DFT, and In Silico Investigation of Two Newly Synthesized β-Diketone Derivatives as Potent COX-2 Inhibitors.Bioengineering (Basel, Switzerland) · 2023Article
- Characterization and Investigation of Novel Benzodioxol Derivatives as Antidiabetic Agents: An In Vitro and In Vivo Study in an Animal Model.Biomolecules · 2023Article
- Article
- Triphenyltin(IV) Carboxylates with Exceptionally High Cytotoxicity against Different Breast Cancer Cell Lines.Biomolecules · 2023Article
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
backgroundNonsteroidal anti-inflammatory drugs (NSAIDs) have been the most commonly used class of medications worldwide for the last three decades.
objectivesThis study aimed to design and synthesize a novel series of methoxyphenyl thiazole carboxamide derivatives and evaluate their cyclooxygenase (COX) suppressant and cytotoxic properties.
methodsThe synthesized compounds were characterized using
resultsThe results revealed that all synthesized molecules have potent inhibitory activities against COX enzymes. The percentage of inhibitory activities at 5 µM concentration against the COX2 enzyme was in the range of 53.9-81.5%, while the percentage against the COX-1 enzyme was 14.7-74.8%. That means almost all of our compounds have selective inhibition activities against the COX-2 enzyme, and the most selective compound was 2f, with selectivity ratio (SR) value of 3.67 at 5 µM concentration, which has a bulky group of trimethoxy on the phenyl ring that could not bind well with the COX-1 enzyme. Compound 2h was the most potent, with an inhibitory activity percentage at 5 µM concentration of 81.5 and 58.2% against COX-2 and COX-1, respectively. The cytotoxicity of these compounds was evaluated against three cancer cell lines: Huh7, MCF-7, and HCT116, and negligible or very weak activities were observed for all of these compounds except compound 2f, which showed moderate activities with IC
conclusionIn general, the series of the synthesized compounds had a strong effect on both enzymes (COX-1 and COX-2) and the trimethoxy compound 2f was more selective than the other compounds.
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