ArticleJournal of advanced research2020
Development of a novel thymidylate synthase (TS) inhibitor capable of up-regulating P53 expression and inhibiting angiogenesis in NSCLC.
Article in Journal of advanced research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 21 citations in OpenAlex.
- Bridging mechanism and design: modern medicinal chemistry approaches to thymidylate synthase inhibitors.RSC advances · 2026Review
- Effect of Concentration of TiOJournal of fluorescence · 2025Article
- Pyrimidine hybrids withFuture medicinal chemistry · 2025Review
- An insight into thymidylate synthase inhibitor as anticancer agents: an explicative review.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- Unveiling the oncogenic significance of thymidylate synthase in human cancers.American journal of translational research · 2024Article
- The anticancer therapeutic potential of pyrimidine-sulfonamide hybrids.Future medicinal chemistry · 2024Review
- An Understanding of Mechanism-Based Approaches for 1,3,4-Oxadiazole Scaffolds as Cytotoxic Agents and Enzyme Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Does Molecular Profiling ofCurrent oncology (Toronto, Ont.) · 2022Article
- Graphene quantum dots rescue angiogenic retinopathy via blocking STAT3/Periostin/ERK signaling.Journal of nanobiotechnology · 2022Article
- Synthesis and Biological Evaluation of 1,2,3-Triazole Tethered Thymol-1,3,4-Oxadiazole Derivatives as Anticancer and Antimicrobial Agents.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Synthesis of New 1, 3, 4-Oxadiazole-Incorporated 1, 2, 3-Triazole Moieties as Potential Anticancer Agents Targeting Thymidylate Synthase and Their Docking Studies.Pharmaceuticals (Basel, Switzerland) · 2020Article
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
introductionThe development of a new type of Thymidylate synthase (TS) inhibitor that could inhibit cancer cells' proliferation and anti-angiogenesis is of great significance for cancer's clinical treatment.
objectivesOur research hopes to develop a TS inhibitor that is more effective than the current first-line clinical treatment of pemetrexed (PTX) and provide a new reference for the clinical treatment of non-small cell lung cancer (NSCLC).
methodsWe obtained a series of novel TS inhibitors by chemical synthesis. Moreover, TS assay and molecular docking to verify the target compound's inhibitory mode. Use MTT assay, colony-forming assay, flow cytometry, and western blot to verify the compound's inhibitory effect on cancer cell proliferation and its mechanism; and explore the compound's effect on angiogenesis
resultsA series of N-(3-(5-phenyl-1,3,4-oxadiazole-2-yl) phenyl)-2,4-dihydroxypyrimidine-5-sulfamide derivatives were synthesized as TS inhibitors for the first time. All target compounds significantly inhibited hTS enzyme activity and demonstrated significant antitumor activity against five cancer cell lines. Notably, 7
conclusionThe anti-angiogenic effect of 7
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Registered trials
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