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Updated: Sep 11, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
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Facile Preparation of 4-Substituted Quinazoline Derivatives

Published on: February 15, 2016

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Synthesis and Evaluation of 2‑Substituted Quinazolin-4(3H)‑ones as Potential Antileukemic Agents

Giorgio Antoniolli1, Keli Lima2, Gilberto Carlos Franchi3

  • 1Institute of Chemistry, University of Campinas, Campinas, SP 13083-862, Brazil.

ACS Omega
|August 18, 2025
PubMed

Insights

Novel quinazolinone derivatives show promise as targeted therapies for acute leukemias. Compounds 6 and 17 demonstrated significant cytotoxic effects against T cell acute lymphoblastic leukemia and acute myeloid leukemia cell lines.

Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Cancer Biology

Background:

  • Rising cancer prevalence and aging populations necessitate novel therapeutic strategies.
  • Acute leukemias (ALL, AML) are aggressive, with poor outcomes, especially in elderly patients.
  • Chemotherapy resistance and toxicity drive the search for new antitumor agents.

Purpose of the Study:

  • To synthesize and evaluate novel 2-substituted quinazolin-4-(3H)-one derivatives as potential anticancer agents.
  • To investigate the cytotoxic activity of these compounds against acute leukemia cell lines.
  • To explore the therapeutic potential of promising candidates for lymphoid and myeloid leukemias.

Main Methods:

  • Synthesis of 20 quinazolinone derivatives via condensation reactions.
  • Characterization using IR, 1H NMR, and 13C NMR spectroscopy.
  • In vitro biological evaluation including cytotoxicity assays (IC50), apoptosis, and cell cycle analysis.

Main Results:

  • Compounds 6 and 17 exhibited potent cytotoxic effects against Jurkat (T cell ALL) and NB4 (APL) cells.
  • Compound 17 showed IC50 values below 5 μM in both cell lines.
  • Compound 6 displayed selectivity towards Jurkat cells, with further in vitro analyses confirming therapeutic potential.

Conclusions:

  • The synthesized quinazolin-4-(3H)-one derivatives, particularly compounds 6 and 17, show significant promise for treating acute leukemias.
  • These findings support further in vivo investigation for the application of quinazolinones in lymphoid and myeloid leukemias.
  • The study highlights the potential of quinazolinone scaffolds in developing targeted therapies for aggressive hematological malignancies.

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