ArticlePharmaceuticals (Basel, Switzerland)2022
Synthesis, Biological Activity, and Molecular Modelling Studies of Naphthoquinone Derivatives as Promising Anticancer Candidates Targeting COX-2.
Article in Pharmaceuticals (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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10 citing papers in PubMed, 20 citations in OpenAlex.
- Synthesis and Development of 3-((2,4-Difluorophenyl)Amino)Propanoic Acid Derivatives as an Antiproliferative Medicinal Chemistry Scaffold Targeting Growth Factor Receptors.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Mechanistic Insights into the Anticancer Action of Novel 2‑Hydroxy-1,4-naphthoquinone Thiol Derivatives.ACS omega · 2025Article
- Synthesis and Biological Evaluation ofMolecules (Basel, Switzerland) · 2025Article
- Identification of 3-[(4-Acetylphenyl)(4-Phenylthiazol-2-Yl)Amino]Propanoic Acid Derivatives as Promising Scaffolds for the Development of Novel Anticancer Candidates Targeting SIRT2 and EGFR.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Dual Anti-Inflammatory and Anticancer Activity of Novel 1,5-Diaryl Pyrazole Derivatives: Molecular Modeling, Synthesis, In Vitro Activity, and Dynamics Study.Biomedicines · 2024Article
- Article
- Natural fulvic acids inhibit non-small-cell lung cancer through the COX-2/PGE2/EP4 axis: In silico and in vivo assessments.Heliyon · 2023Article
- Biological Activity of Naphthoquinones Derivatives in the Search of Anticancer Lead Compounds.Toxins · 2023Article
- Cyclooxygenase-2 (COX-2) as a Target of Anticancer Agents: A Review of Novel Synthesized Scaffolds Having Anticancer and COX-2 Inhibitory Potentialities.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Antioxidant and Anticancer Potential of Bioactive Compounds fromPlants (Basel, Switzerland) · 2022Article
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Authors and funding
9 authors at 5 institutions in 4 countries.
Funding
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Abstract
Non-small cell lung cancer (NSCLC) remains a leading cause of cancer-associated mortalities worldwide. Therefore, it is crucial to develop a novel therapeutic option targeting localized and metastatic NSCLC. In this paper, we describe the synthesis and biological activity characterization of naphthoquinone derivatives bearing selective anticancer activity to NSCLC via a COX-2 mediated pathway. The biological evaluation of compounds 9−16 showed promising structure-dependent anticancer activity on A549 cells in 2D and 3D models. Compounds were able to significantly (p < 0.05) reduce the A549 viability after 24 h of treatment in comparison to treated control. Compounds 9 and 16 bearing phenylamino and 4-hydroxyphenylamino substituents demonstrated the most promising anticancer activity and were able to induce mitochondrial damage and ROS formation. Furthermore, most promising compounds showed significantly lower cytotoxicity to non-cancerous Vero cells. The in silico ADMET properties revealed promising drug-like properties of compounds 9 and 16. Both compounds demonstrated favorable predicted GI absorption values, while only 16 was predicted to be permeable through the blood−brain barrier. Molecular modeling studies identified that compound 16 is able to interact with COX-2 in arachidonic acid site. Further studies are needed to better understand the safety and in vivo efficacy of compounds 9 and 16.
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