ArticleBioorganic & medicinal chemistry2013
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells.
Article in Bioorganic & medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 44 citations in OpenAlex.
- Unlocking the potential: unveiling tyrphostins with Michael-reactive cyanoacrylate motif as promising inhibitors of human 5-lipoxygenase.Pflugers Archiv : European journal of physiology · 2024Article
- Synthesis, Evaluation of Enzyme Inhibition and Redox Properties of Potential Dual COX-2 and 5-LOX Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Integracides: Tetracyclic Triterpenoids fromLife (Basel, Switzerland) · 2022Article
- Design, Synthesis, and Biological Evaluation of Novel N-Acylhydrazone Bond Linked Heterobivalent β-Carbolines as Potential Anticancer Agents.Molecules (Basel, Switzerland) · 2019Article
- Derivatives of a benzoquinone acyl hydrazone with activity against Toxoplasma gondii.International journal for parasitology. Drugs and drug resistance · 2018Article
- Association of Single-Nucleotide Polymorphisms of CD44 Gene with Susceptibility to Breast Cancer in Chinese Women.Medical science monitor : international medical journal of experimental and clinical research · 2018Article
- Novel Toxoplasma gondii inhibitor chemotypes.Parasitology international · 2018Article
- Review
- Transforming growth factor β1 (TGFβ1)-induced CD44V6-NOX4 signaling in pathogenesis of idiopathic pulmonary fibrosis.The Journal of biological chemistry · 2017Article
- Roles of Proteoglycans and Glycosaminoglycans in Wound Healing and Fibrosis.International journal of cell biology · 2015Review
- Isothiocyanate analogs targeting CD44 receptor as an effective strategy against colon cancer.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2014Article
- Periostin induces intracellular cross-talk between kinases and hyaluronan in atrioventricular valvulogenesis.The Journal of biological chemistry · 2014Article
- Overexpression of c-Met and CD44v6 receptors contributes to autocrine TGF-β1 signaling in interstitial lung disease.The Journal of biological chemistry · 2014Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
Abstract
Cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) enzyme have been found to play a role in promoting growth in colon cancer cell lines. The di-tert-butyl phenol class of compounds has been found to inhibit both COX-2 and 5-LOX enzymes with proven effectiveness in arresting tumor growth. In the present study, the structural analogs of 2,6 di-tert-butyl-p-benzoquinone (BQ) appended with hydrazide side chain were found to inhibit COX-2 and 5-LOX enzymes at micromolar concentrations. Molecular docking of the compounds into COX-2 and 5-LOX protein cavities indicated strong binding interactions supporting the observed cytototoxicities. The signaling interaction between endogenous hyaluronan and CD44 has been shown to regulate COX-2 activities through ErbB2 receptor tyrosine kinase (RTK) activation. In the present studies it has been observed for the first time, that three of our COX/5-LOX dual inhibitors inhibit proliferation upon hydrazide substitution and prevent the activity of pro-angiogenic factors in HCA-7, HT-29, Apc10.1 cells as well as the hyaluronan synthase-2 (Has2) enzyme over-expressed in colon cancer cells, through inhibition of the hyaluronan/CD44v6 cell survival pathway. Since there is a substantial enhancement in the antiproliferative activities of these compounds upon hydrazide substitution, the present work opens up new opportunities for evolving novel active compounds of BQ series for inhibiting colon cancer.
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