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  • Chem Sci Trans., 2014, 3(4),  pp 1562-1568  

    DOI:10.7598/cst2014.896

    Research Article

    3-[(E)-(4-Hydroxy-3-methoxybenzylidene)amino]-2-thioxoimidazolidin-4-one as Snail1 Inhibitor with Anticancer and Anti-migratory Properties Against Colorectal Cancer

  • DHANYA SUNIL*, C. RANJITHA1 and M. RAMA and S. BALAJI
  • Department of Chemistry, Department of Biotechnology, Manipal Institute of Technology, Manipal University- 576 104, India
  • Abstract

    Colorectal cancer is the third leading cause of cancer related deaths in humans. Research is going on to increase the treatment options of colon cancer with decreased side effects. Four imidazolidinones were synthesized by the cyclization reaction between Schiff bases and ethylchloroacetate and were characterized by advanced spectral techniques and CHN analysis. The cytotoxic and anti-migratory properties of imidazolidinones against HCT116 (human colorectal adenocarcinoma) cells were studied using Sulphorhodamine-B (SRB) assay and wound healing assay respectively. 3-[(E)-(4-Hydroxy-3-methoxybenzylidene)amino]-2-thioxoimidazolidin-4-one (2d) displayed excellent cytotoxicity with low IC50 in SRB assay. The wound gap observed on treatment with 2d indicated the reduced motility of HCT116 cells. Snail1, an E-Cadherin repressor plays an important role in epithelial to mesenchymal transition which influences metastatic cancer and hence, a molecular target in cancer treatment for anti-invasive drugs. The effective binding of 2d into the active site of snail1 in docking studies, suggests it to be a promising anti-neoplastic agent in the treatment of colorectal cancer.

    Keywords

    Oxazepines, Cytotoxicity, Metastases, Snail1

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