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Exploration of the VEGFR-2 inhibition activity of phthalazine derivatives: design, synthesis, cytotoxicity, ADMET,

Hatem Hussein Bayoumi1, Mohamed-Kamal Ibrahim1, Mohammed A Dahab1

  • 1Pharmaceutical Medicinal Chemistry and Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University Nasr City 11884 Cairo Egypt eladlkhaled74@yahoo.com eladlkhaled74@azhar.edu.eg khaled.eladl@hu.edu.eg.

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This summary is machine-generated.

Novel phthalazine derivatives show potent anticancer activity by inhibiting VEGFR-2. Compounds 2g and 4a were most effective against breast and liver cancer cell lines, demonstrating promising therapeutic potential.

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) is a key target in cancer therapy.
  • Developing novel inhibitors is crucial for overcoming drug resistance and improving treatment efficacy.
  • Phthalazine scaffolds offer a promising structural basis for designing new anticancer agents.

Purpose of the Study:

  • To design, synthesize, and evaluate novel phthalazine derivatives as VEGFR-2 inhibitors.
  • To assess the in vitro anticancer activity of these compounds against human breast (MCF-7) and liver (Hep G2) cancer cell lines.
  • To investigate the correlation between biological activity and molecular modeling predictions.

Main Methods:

  • Synthesis of novel phthalazine derivatives.
  • In vitro cytotoxicity assays against MCF-7 and Hep G2 cell lines.
  • Enzyme inhibition assays against VEGFR-2.
  • Molecular docking and molecular dynamics (MD) simulations.
  • In silico ADMET profiling.

Main Results:

  • Compounds 2g and 4a exhibited potent inhibition of VEGFR-2 with IC50 values of 0.148 μM and 0.196 μM, respectively.
  • These compounds also demonstrated significant anticancer activity against MCF-7 and Hep G2 cell lines, with IC50 values as low as 0.09 μM.
  • Biological data strongly correlated with molecular modeling results, and MD simulations confirmed stable ligand-target interactions.
  • Derivatives 2g and 4a displayed favorable in silico ADMET properties.

Conclusions:

  • Novel phthalazine derivatives are effective VEGFR-2 inhibitors with significant anticancer potential.
  • Compounds 2g and 4a represent promising lead candidates for further development in cancer therapy.
  • The study highlights the utility of integrated biological and computational approaches in drug discovery.