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<p>The rising incidence of cancer necessitates the development of novel therapeutic agents with targeted action. This study focuses on the synthesis and characterization of imidazolidinedione analogues, a class of compounds known for their diverse biological activities. We synthesized a series of imidazolidinedione analogues using a streamlined synthetic approach, followed by comprehensive characterization using spectroscopic techniques, including IR, NMR, and mass spectrometry. A molecular docking study was performed to coordinate its binding affinity towards COX-2. In vitro assays were performed to determine the anticancer effects of the synthesized analogues on cancer cell lines. The DPPH scavenging assay was performed for in vitro antioxidant activity, with ascorbic acid as the reference standard. Our findings indicate that the imidazolidinedione analogues (5a-5e) exhibit significant COX-2 inhibition and show promising anticancer activity. Compound 5e showed the IC<sub>50</sub> value of 200&#xa0;nm, suggesting their potential as effective therapeutic agents towards cancer cell lines. It also showed an antiangiogenic effect in the chorioallantoic membrane (CAM) assay. This study highlights the importance of imidazolidinedione derivatives in the development of targeted cancer therapies and paves the way for further research into their mechanisms of action and therapeutic applications.</p> Graphical Abstract <p></p>

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Design, and Synthesis of Novel Imidazolidinedione Derivatives: Exploring their Anticancer Potential, Angiogenesis and in Silico Study Towards COX-2

  • 期刊论文

  • 发表日期：

    2025年8月22日

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  • Smriti Dewangan,
  • Alok Singh Thakur,
  • Aruna Ghose,
  • Moonmun Dhara,
  • Anchal Verma,
  • Varsha Rawat,
  • Shakti Ketan Prusty,
  • Gregory Smith

摘要

The rising incidence of cancer necessitates the development of novel therapeutic agents with targeted action. This study focuses on the synthesis and characterization of imidazolidinedione analogues, a class of compounds known for their diverse biological activities. We synthesized a series of imidazolidinedione analogues using a streamlined synthetic approach, followed by comprehensive characterization using spectroscopic techniques, including IR, NMR, and mass spectrometry. A molecular docking study was performed to coordinate its binding affinity towards COX-2. In vitro assays were performed to determine the anticancer effects of the synthesized analogues on cancer cell lines. The DPPH scavenging assay was performed for in vitro antioxidant activity, with ascorbic acid as the reference standard. Our findings indicate that the imidazolidinedione analogues (5a-5e) exhibit significant COX-2 inhibition and show promising anticancer activity. Compound 5e showed the IC50 value of 200 nm, suggesting their potential as effective therapeutic agents towards cancer cell lines. It also showed an antiangiogenic effect in the chorioallantoic membrane (CAM) assay. This study highlights the importance of imidazolidinedione derivatives in the development of targeted cancer therapies and paves the way for further research into their mechanisms of action and therapeutic applications.

Graphical Abstract