Russian Journal of General Chemistry

, Volume 89, Issue 8, pp 1683–1690 | Cite as

New Pyridopyrimidone Derivatives: Synthesis, Molecular Docking Studies, and Potential Anticancer Activity

  • N. M. KhalifaEmail author
  • H. M. Alkahtani
  • M. A. Al-Omar
  • A. H. Bakheit


A new series of pyrido[2,3-d]pyrimidones incorporated pyrazoles and fused triazoles are synthesized and tested in vitro for cytotoxic effect against cancer cell lines: HePG-2, HCT-116, MCF-7, PC-3, and A-549. Their inhibition of protein kinase is assessed. The highest growth inhibitory (IC50 0.3 µM) effect is determined for one of compounds as compared with doxorubicin (IC50 0.6 µM). A modeling study is performed for approaching the compounds mode of binding and their similarity with the positive control drugs.


pyridopyrimidones cytotoxic agents molecular docking 


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The project was financially supported by King Saud University, Vice Deanship of Research Chairs.


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Copyright information

© Pleiades Publishing, Ltd. 2019

Authors and Affiliations

  • N. M. Khalifa
    • 1
    • 2
    Email author
  • H. M. Alkahtani
    • 3
  • M. A. Al-Omar
    • 1
    • 3
  • A. H. Bakheit
    • 3
    • 4
  1. 1.Pharmaceutical Chemistry Department, Drug Exploration and Development Chair (DEDC), College of PharmacyKing Saud UniversityRiyadhSaudi Arabia
  2. 2.Therapeutic Chemistry Department, Pharmaceutical and Drug Industries DivisionNational Research CentreGiza, CairoEgypt
  3. 3.Pharmaceutical Chemistry Department, College of PharmacyKing Saud UniversityRiyadhSaudi Arabia
  4. 4.Chemistry Department, Faculty of Science and TechnologyAl-Neelain UniversityKhartoumSudan

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