2. Academic Validation
  3. Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line

Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line

  • Eur J Med Chem. 2018 Aug 5:156:563-579. doi: 10.1016/j.ejmech.2018.07.003.
Islam Zaki 1,  Mohammed K Abdelhameid 2,  Ibrahim M El-Deen 3,  Abdel Hady A Abdel Wahab 4,  Abeer M Ashmawy 4,  Khaled O Mohamed 5
Affiliations

Affiliations

  • 1 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, Egypt.
  • 2 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt. Electronic address: mohorganic@hotmail.com.
  • 3 Chemistry Department, Faculty of Science, Port Said University, Port Said, Egypt.
  • 4 Cancer Biology Department, National Cancer Institute, Cairo University, Cairo, Egypt.
  • 5 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
PMID: 30025350 DOI: 10.1016/j.ejmech.2018.07.003
Abstract

Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent Anticancer activity over MCF-7 breast Cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, 4c, 5e, 6c and 7c show a potent inhibitory activity of cell proliferation and cell cycle arrest at G2/M phase. Compounds 4c, 5e and 7c exhibit low to moderate β-tubulin polymerization inhibition percentage. Meanwhile, compound 6c displayed excellent β-tubulin percentage of polymerization inhibition equivalent to that exhibited by podo. In addition, compounds 4c, 5e and 7c show strong Topoisomerase (topo) II inhibitory activity in nano-molar concentration, compared to known topo inhibitor as etoposide. Finally, apoptotic inducing activity over MCF-7 of compounds 4c, 5e, 6c and 7c is due to up-regulation of p53, increased Bax/Bcl-2 ratio and caspase3/7 levels 2-fold higher than podo.

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