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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

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Synthesis, In Vitro Anticancer Activity, Molecular Docking, and Dynamic Simulation Study of Thiazole-Conjugated

Deepali M Wanode¹, Pramod B Khedekar¹, Somdatta Y Chaudhari²

¹Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur, Maharashtra, India.

Chemistry & Biodiversity

|June 3, 2025

Summary

Novel thiazole-pyrazole hybrid compounds were synthesized and tested for anticancer activity against breast cancer. Compound IVc showed promising results, indicating potential for new breast cancer therapeutics.

Keywords:

ADMET cancer molecular docking molecular dynamics simulation pyrazole thiazole

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Area of Science:

Medicinal Chemistry
Organic Synthesis
Pharmacology

Background:

Breast cancer remains a leading cause of mortality worldwide, necessitating the development of novel therapeutic agents.
Hybridization of pharmacophores is a strategic approach to discover compounds with enhanced biological activity.
Thiazole and pyrazole moieties are recognized for their diverse pharmacological properties, including anticancer effects.

Purpose of the Study:

To design and synthesize novel hybrid compounds incorporating thiazole and pyrazole pharmacophores.
To evaluate the in vitro anticancer activity of these hybrids against the MCF-7 breast cancer cell line.
To investigate the molecular interactions and pharmacokinetic properties of the most potent compounds.

Main Methods:

Synthesis of hybrid compounds utilizing the Vilsmeier-Haack reaction.
Structural elucidation through FTIR, 1H NMR, 13C NMR, and high-resolution mass spectrometry (HRMS).
In vitro anticancer activity assessment using the MCF-7 cell line and determination of IC50 values.
Molecular docking studies targeting VEGFR-2 kinase and molecular dynamic simulations.
ADMET (Absorption, Distribution, Metabolism, Excretion, Toxicity) predictions for pharmacokinetic profiling.

Main Results:

Successful synthesis and characterization of novel thiazole-pyrazole hybrid compounds.
Compound IVc demonstrated significant in vitro anticancer activity against MCF-7 cells, with an IC50 of 126.98 µM.
Molecular docking and simulations revealed stable interactions of compound IVc with VEGFR-2 kinase.
ADMET predictions indicated favorable pharmacokinetic properties, suggesting good drug-likeness.

Conclusions:

The synthesized thiazole-pyrazole hybrids represent a promising class of compounds for breast cancer treatment.
Compound IVc exhibits notable anticancer potential warranting further investigation.
This study provides a foundation for the rational design of novel anticancer agents based on thiazole-pyrazole scaffolds.