Design, synthesis and antitumor activity of novel pyran-functionalized uracil derivatives: docking studies

Faculty Science Year: 2023
Type of Publication: ZU Hosted Pages:
Authors:
Wael Shehta Metwally Elsayed Azab
Journal: Future Medicinal Chemistry Future Science and Newlands Press Volume: 15
Keywords : Design, synthesis , antitumor activity , novel pyran-functionalized    
Abstract:
Aim: Synthesis of novel pyran-based uracils that may have potent antitumor activity against hepatocellular carcinoma HepG2 and ovarian cancer SKOV3 cell lines. Materials & methods: Novel pyran-based uracils were synthesized and their anticancer activity was assessed using methyl thiazolyl tetrazolium and wound-healing assays to detect their cytotoxicity and their antiproliferative and antimigratory activities. Results: Compounds 3, 5, 6, 7, 8, 9, 10, 11 and 13 significantly inhibited cell proliferation of the HepG2 cell line. Compounds 7, 8, 9 and 13 significantly inhibited the proliferation of SKOV3 cells, which was also proven through docking studies with topoisomerase I. Conclusion: The molecular docking analysis revealed that 7 and 9 are two major compounds found to possess higher degrees of interaction with DNA gyrase.
    
     
 
       

Author Related Publications

  • Wael Shehta Metwally Elsayed Azab, "Utility of 2-furan-2-yl-4-mercapto-6-methylpyrimidine-5-carbonitrile as a precursor for the synthesis of some novel pyrimidines: Antibacterial activity", SPRINGER, 2018 More
  • Wael Shehta Metwally Elsayed Azab, "Cyclization of mercaptopyrimidine derivative: A facile synthetic approach for condensed pyrimidines", Springer nature, 2018 More
  • Wael Shehta Metwally Elsayed Azab, "Synthesis and Antibacterial Acivity of Some Novel Pyrimidine-Based Heterocycles", Pleiades Publishing, 2019 More
  • Wael Shehta Metwally Elsayed Azab, "Heterocyclization of a thiouracil derivative as a synthetic entry to novel condensed pyrimidines of biological interest", Pleiades Publishing, 2020 More
  • Wael Shehta Metwally Elsayed Azab, "Design and synthesis of fused and spiro pyrazole derivatives", Pleiades Publishing, 2020 More

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