ArticleChemical biology & drug design2022
1,3-diarylpyrazolones as potential anticancer agents for non-small cell lung cancer: Synthesis and antiproliferative activity evaluation.
Article in Chemical biology & drug design, 2022. 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, 10 citations in OpenAlex.
- The Pyrazolone Scaffold: A Privileged Motif for Molecular Hybridization in Drug Discovery.ChemMedChem · 2026Review
- Isoselenourea-Catalyzed Enantioselective Pyrazolo-Heterocycle Synthesis Enabled by Self-Correcting Amide and Ester Acylation.Angewandte Chemie (International ed. in English) · 2025Article
- Recent advances in the synthesis of anticancer pyrazole derivatives using microwave, ultrasound, and mechanochemical techniques.RSC advances · 2025Review
- Synthesis,Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Pyrazolone-type compounds (part II):RSC advances · 2023Article
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Authors and funding
7 authors at 1 institution in 1 country.
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Abstract
A series of pyrazolone compounds with different substitution patterns have been synthesized using microwave-assisted methods and evaluated their in vitro antiproliferative activity against human lung adenocarcinoma cell lines (A549 and NCI-H522). Among the tested compounds, the pyrazolone P7 exhibited high antiproliferative activity against both A549 and NCIH522 cancer cell lines while being 10 times less cytotoxic to non-cancerous cells. Moreover, our compounds P7 and P11 exhibited higher antiproliferative activity and selectivity against A549 and NCIH522 cells compared with the clinically approved drugs Afatinib and Gefitinib. The cell cycle analysis showed that the compound P7 and P11 arrests the cell cycle at G0/G1 phase, whereas the compounds P13 and P14 involved in G2/M phase arrest. The results from antiproliferative activity screening, cell cycle analysis, and kinase profiling indicate that the suitably substituted 1,3-diarylpyrazolones exhibit high antiproliferative activity against non-small cell lung cancer cells.
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Registered trials
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