Advances in Hydrazone Compounds with Anticancer Activity

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 25 November 2025 | Viewed by 645

Special Issue Editors


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Guest Editor
Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria
Interests: hydrazones; anticancer activity; metal complexes; lipophilicity; structure–activity relations

E-Mail Website
Guest Editor
Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria
Interests: drug design; molecular docking; molecular dynamics; hydrazones; anticancer activity; structure–activity relations
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Special Issue Information

Dear Colleagues,

Hydrazones, characterized by their R-C=N-NH-R' linkage, are attracting widespread attention in medicinal chemistry as a promising class of anticancer agents. Their structural simplicity, synthetic accessibility, and diverse pharmacological activities have prompted extensive research into their anticancer potential. One important trend in this domain is the development of novel hydrazone derivatives with enhanced potency and selectivity, with structural modifications—such as the incorporation of heterocyclic rings, introduction of halogen atoms, and optimization of substituent groups, including methoxy, methyl, and amino groups—serving as strategies. Another means by which to increase activity is to include hydrazones as ligands in various metal complexes. A key area of research is therefore understanding their mechanisms of action. The conjugation of hydrazones with nanoparticles is also being examined to ensure the precise targeting of the tumor while minimizing systemic toxicity and maximizing therapeutic concentration at target sites.

This Special Issue focuses on advances in the design, synthesis, and anticancer activity of novel hydrazones and their metal complexes. Authors are encouraged to contribute original research articles, reviews, and short communications examining hydrazones that selectively target specific cancer hallmarks, leading to improved efficacy and reduced off-target effects.

Dr. Boryana Nikolova-Mladenova
Prof. Dr. Mariyana Atanasova
Guest Editors

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Keywords

  • hydrazones
  • lipophilicity
  • logP
  • anticancer activity
  • selectivity

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Published Papers (1 paper)

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Research

24 pages, 1620 KB  
Article
Novel Indole-Based Sulfonylhydrazones as Potential Anti-Breast Cancer Agents: Synthesis, In Vitro Evaluation, ADME, and QSAR Studies
by Violina T. Angelova, Rositsa Mihaylova, Zvetanka Zhivkova, Nikolay Vassilev, Boris Shivachev and Irini Doytchinova
Pharmaceuticals 2025, 18(8), 1231; https://doi.org/10.3390/ph18081231 - 20 Aug 2025
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Abstract
Background: Breast cancer continues to pose a significant global health challenge despite advances in early detection and targeted therapies. The development of novel chemotherapeutic agents remains crucial, particularly those with selective cytotoxicity toward specific breast cancer subtypes. Methods: A series of [...] Read more.
Background: Breast cancer continues to pose a significant global health challenge despite advances in early detection and targeted therapies. The development of novel chemotherapeutic agents remains crucial, particularly those with selective cytotoxicity toward specific breast cancer subtypes. Methods: A series of ten hybrid indolyl-methylidene phenylsulfonylhydrazones and one bis-indole derivative were designed, synthesized, and structurally characterized using NMR and high-resolution mass spectrometry (HRMS). Prior to synthesis, in silico screening was performed to assess drug likeness and ADME-related properties. Single-crystal X-ray diffraction was conducted for compound 3e. The cytotoxic potential of the synthesized compounds was evaluated using the MTT assay against MCF-7 (ER-α⁺) and MDA-MB-231 (triple-negative) breast cancer cell lines. Additionally, quantitative structure–activity relationship (QSAR) analysis was conducted to identify key structural features contributing to activity. Results: Most compounds exhibited selective cytotoxicity against MCF-7 cells. Notably, compound 3b demonstrated the highest potency with an IC50 of 4.0 μM and a selectivity index (SI) of 20.975. Compound 3f showed strong activity against MDA-MB-231 cells (IC50 = 4.7 μM). QSAR analysis revealed that the presence of a non-substituted phenyl ring and specific indolyl substituents (5-methoxy, 1-acetyl, 5-chloro) significantly contributed to enhanced cytotoxic activity and ligand efficiency. Conclusion: The synthesized phenylsulfonylhydrazone hybrids exhibit promising and selective cytotoxicity, particularly against ER-α⁺ breast cancer cells. Structural insights from QSAR analysis provide a valuable foundation for the further optimization of this scaffold as a potential source of selective anticancer agents. Full article
(This article belongs to the Special Issue Advances in Hydrazone Compounds with Anticancer Activity)
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