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Novel benzimidazole-based thioamide derivatives as potential anticancer agents: synthesis, biological evaluation, and

Mahadevi Vitthal Kendre1, Sachin S Bhusari1, Pravin S Wakte1

  • 1Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Chhatrapati Sambhajinagar, MS 431004, India.

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|March 29, 2026
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Summary

Novel benzimidazole thioamides show potent anticancer activity against lung and liver cancer cell lines. Molecular docking suggests these compounds may target the mutated epidermal growth factor receptor (EGFR), warranting further investigation.

Keywords:
Anticancer activityBenzimidazole-based thioamide derivativesDrug-likenessEGFR inhibitionMolecular dockingNitrobenzyl compoundsStructure-activity relationship (SAR)

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Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Cancer Research

Background:

  • Benzimidazole derivatives are recognized for diverse biological activities.
  • Targeting mutated epidermal growth factor receptor (EGFR) is a key strategy in cancer therapy.
  • Developing novel anticancer agents with improved efficacy and specificity is crucial.

Purpose of the Study:

  • To design, synthesize, and evaluate novel benzimidazole-based thioamide derivatives for anticancer potential.
  • To investigate the EGFR-targeting capabilities of these compounds using molecular docking.
  • To identify lead compounds for further anticancer drug development.

Main Methods:

  • Synthesis of benzimidazole-based thioamide derivatives via base-mediated nucleophilic substitution.
  • Optimization of reaction conditions (solvent, base, temperature) for efficient synthesis.
  • In vitro cytotoxic evaluation against human cancer cell lines (MCF7, A-549, HEP-G2).
  • Molecular docking studies against T790M-mutated EGFR kinase domain.
  • ADME predictions using Qikprop.

Main Results:

  • Ten novel benzimidazole-based thioamide derivatives were successfully synthesized and characterized.
  • Compounds 6-8b demonstrated significant in vitro cytotoxic activity, with IC₅₀ values as low as 3.70 μM against A-549 cells.
  • Molecular docking revealed favorable binding interactions with the T790M-mutated EGFR, outperforming the reference inhibitor Neratinib.
  • ADME predictions provided insights into pharmacokinetic properties.

Conclusions:

  • The synthesized benzimidazole-based thioamide derivatives exhibit promising anticancer activity.
  • These compounds represent a potential lead scaffold for developing EGFR-targeted anticancer agents.
  • Further mechanistic studies and experimental validation of EGFR target engagement are necessary.