ArticleEuropean journal of medicinal chemistry2012
From COX-2 inhibitor nimesulide to potent anti-cancer agent: synthesis, in vitro, in vivo and pharmacokinetic evaluation.
Article in European journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
24 citing papers in PubMed.
- Synthesis, characterization, biological evaluation, and molecular modeling of novel nimesulide urea derivatives as potential MetAP2 inhibitors.Scientific reports · 2026Article
- Enzyme-Targeted Antiproliferative Effects of Novel Indole-Acrylamide Xenobiotics Acting on Cyclooxygenase Pathways.Journal of xenobiotics · 2026Article
- Nimesulide Containing Dimethoxy Benzamide: From Fever Reduction to Cancer Treatment.ACS omega · 2025Article
- Repurposing of Indomethacin and Naproxen as anticancer agents: progress from 2017 to present.RSC advances · 2024Review
- Heat shock proteins as hallmarks of cancer: insights from molecular mechanisms to therapeutic strategies.Journal of hematology & oncology · 2024Review
- Recent Advancements in Refashioning of NSAIDs and their Derivatives as Anticancer Candidates.Current pharmaceutical design · 2024Review
- Mass balance, metabolic disposition, and pharmacokinetics of a single IV dose of [14C]CA102N in HT-29 xenograft athymic nude mice.Frontiers in pharmacology · 2024Article
- Nimesulide, a COX-2 inhibitor, sensitizes pancreatic cancer cells to TRAIL-induced apoptosis by promoting DR5 clustering †.Cancer biology & therapy · 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
- More Than Resveratrol: New Insights into Stilbene-Based Compounds.Biomolecules · 2020Review
- Mixed-Generation PAMAM G3-G0 Megamer as a Drug Delivery System for Nimesulide: Antitumor Activity of the Conjugate Against Human Squamous Carcinoma and Glioblastoma Cells.International journal of molecular sciences · 2019Article
- Synthesis and Different Effects of Biotinylated PAMAM G3 Dendrimer Substituted with Nimesulide in Human Normal Fibroblasts and Squamous Carcinoma Cells.Biomolecules · 2019Article
- Design, Synthesis and Biological Evaluation of Novel 4-Substituted Coumarin Derivatives as Antitumor Agents.Molecules (Basel, Switzerland) · 2018Article
- Effects of celecoxib on cell apoptosis and Fas, FasL and Bcl-2 expression in a BGC-823 human gastric cancer cell line.Experimental and therapeutic medicine · 2017Article
- Synthesis and biological evaluation of selective tubulin inhibitors as anti-trypanosomal agents.Bioorganic & medicinal chemistry · 2017Article
- Challenges in the chemotherapy of Chagas disease: Looking for possibilities related to the differences and similarities between the parasite and host.World journal of biological chemistry · 2017Review
- Hyaluronic acid-nimesulide conjugates as anticancer drugs against CD44-overexpressing HT-29 colorectal cancer in vitro and in vivo.International journal of nanomedicine · 2017Article
- Article
- A Simple and Rapid LC-MS/MS Method for the Determination of BMCL26 a Novel Anti-Parasitic Agent in Rat Plasma.Journal of analytical & bioanalytical techniques · 2015Article
- A New Ligustrazine Derivative-Selective Cytotoxicity by Suppression of NF-κB/p65 and COX-2 Expression on Human Hepatoma Cells. Part 3.International journal of molecular sciences · 2015Article
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Authors and funding
10 authors.
Funding
Abstract
Cyclooxygenase-2 (COX-2) inhibitor nimesulide inhibits the proliferation of various types of cancer cells mainly via COX-2 independent mechanisms, which makes it a good lead compound for anti-cancer drug development. In the presented study, a series of new nimesulide analogs were synthesized based on the structure-function analysis generated previously. Some of them displayed very potent anti-cancer activity with IC(50)s around 100 nM-200 nM to inhibit SKBR-3 breast cancer cell growth. CSUOH0901 (NSC751382) from the compound library also inhibits the growth of the 60 cancer cell lines used at National Cancer Institute Developmental therapeutics Program (NCIDTP) with IC(50)s around 100 nM-500 nM. Intraperitoneal injection with a dosage of 5 mg/kg/d of CSUOH0901 to nude mice suppresses HT29 colorectal xenograft growth. Pharmacokinetic studies demonstrate the good bioavailability of the compound.
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Registered trials
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