Related Experiment Video

Updated: Jul 20, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
11:51

Facile Preparation of 4-Substituted Quinazoline Derivatives

Published on: February 15, 2016

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The Synthesis and Biological Evaluation of 2-(1H-Indol-3-yl)quinazolin-4(3H)-One Derivatives

Elena Y Mendogralo1, Larisa Y Nesterova1,2, Ekaterina R Nasibullina1

  • 1Department of Chemistry, Perm State University, Bukireva St. 15, 614990 Perm, Russia.

Molecules (Basel, Switzerland)
|July 29, 2023
PubMed

Insights

New indolylquinazolinone compounds show potent antibacterial activity against drug-resistant bacteria like methicillin-resistant Staphylococcus aureus (MRSA). Some compounds also exhibit significant anticancer properties, targeting rapidly dividing cancer cells.

Area of Science:

  • Medicinal Chemistry
  • Antimicrobial Research
  • Cancer Biology

Background:

  • Antibiotic resistance in bacteria, particularly Staphylococcus aureus (including MRSA) and Mycobacterium tuberculosis, poses a significant global health challenge.
  • The development of novel antibacterial agents is crucial to combat resistant infections.

Purpose of the Study:

  • To synthesize and evaluate novel 2-(1H-indol-3-yl)quinazolin-4(3H)-one analogues for their antimicrobial and anticancer activities.
  • To investigate the structure-activity relationships of the synthesized compounds.

Main Methods:

  • Synthesis of 2-(1H-indol-3-yl)quinazolin-4(3H)-one analogues.
  • Antimicrobial susceptibility testing against Mycobacterium tuberculosis, Staphylococcus aureus (MRSA), and Candida albicans.
  • Biofilm inhibition assays for Staphylococcus aureus.
  • Molecular docking studies against RelA/SpoT homolog proteins.
  • Cytotoxicity assays against various cancer cell lines.

Main Results:

  • Compound 3k demonstrated potent activity against MRSA with a minimum inhibitory concentration (MIC) of 0.98 μg/mL.
  • Several synthesized compounds exhibited significant antiproliferative activity against tested cancer cell lines.
  • Compounds 3b, 3e, and 3g selectively inhibited the growth of A549 cancer cells over normal fibroblasts.

Conclusions:

  • The synthesized indolylquinazolinones represent a promising class of compounds with dual potential as antibacterial agents against resistant strains and as anticancer therapeutics.
  • Further research into these compounds could lead to new treatments for bacterial infections and cancer.
Keywords:
Mycobacterium smegmatisantibacterial activityazaheterocycleindolemolecular dockingquinazolinoneresistance

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