Previous Article in Journal
A Comprehensive Approach to the Antidepressant-like Effect and Toxicity of Thunbergia alata Bojer ex Sims (Acanthaceae): Involvement of the Serotoninergic System
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
Pharmaceuticals
Volume 18
Issue 12
10.3390/ph18121813
pharmaceuticals-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
This is an early access version, the complete PDF, HTML, and XML versions will be available soon.
Article

Reinvestigating Pyrrol-2-One-Based Compounds: From Antimicrobial Agents to Promising Antitumor Candidates

by
Natalia Simionescu
1,†,
Ashraf Al-Matarneh
1,2,†,
Ionel I. Mangalagiu
2,
Narcis Cibotariu
1,
Cristina Mariana Uritu
3,
Cristina Maria Al-Matarneh
1,* and
Mariana Pinteala
1
1
Centre of Advanced Research in Bionanoconjugates and Biopolymers, “Petru Poni” Institute of Macrmoleclar Chemistry of Romanian Academy, 41A Grigore Ghica Voda Alley, 700487 Iasi, Romania
2
Faculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, Romania
3
Advanced Center for Research and Development in Experimental Medicine “Prof. Ostin C. Mungiu”, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iasi, Romania
*
Author to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Pharmaceuticals 2025, 18(12), 1813; https://doi.org/10.3390/ph18121813 (registering DOI)
Submission received: 29 October 2025 / Revised: 24 November 2025 / Accepted: 25 November 2025 / Published: 27 November 2025
(This article belongs to the Special Issue Antimicrobial and Anticancer Scaffolds in Medicinal Chemistry)
Browse Figure
Versions Notes

Abstract

Background: Heteroaromatic iodine-containing compounds have been previously recognized for their broad-spectrum antimicrobial activity. This study aims to systematically investigate their potential repurposing as anticancer agents, with a particular focus on understanding the structural determinants that influence their cytotoxicity and selectivity toward malignant cells. Methods: A series of heteroaromatic iodine-containing derivatives were synthesized and evaluated for anticancer activity. Their cytotoxic effects were measured and compared between cancerous and normal cell lines to determine selectivity. Structural features, including heteroaromatic moieties and substituents, were analyzed to identify correlations with biological activity. Results: Among the tested compounds, derivatives 3e, 3g, and 3l demonstrated significant cytotoxic effects while exhibiting favorable selectivity indices. These findings indicate that these compounds preferentially target malignant cells over normal cells, thereby mitigating the issue of systemic toxicity often associated with traditional chemotherapeutics. The enhanced anticancer activity appears to be influenced by specific structural elements within the heteroaromatic framework. Conclusions: The study highlights the potential of heteroaromatic iodine-containing compounds as promising anticancer candidates. Rational structural modifications within these heterocyclic systems can effectively modulate bioactivity and improve therapeutic selectivity. These results support further development of this compound class for anticancer applications.
Keywords: pyrrol-2-one; antitumor activity; iodine; osteosarcoma pyrrol-2-one; antitumor activity; iodine; osteosarcoma
Graphical Abstract

Share and Cite

MDPI and ACS Style

Simionescu, N.; Al-Matarneh, A.; Mangalagiu, I.I.; Cibotariu, N.; Uritu, C.M.; Al-Matarneh, C.M.; Pinteala, M. Reinvestigating Pyrrol-2-One-Based Compounds: From Antimicrobial Agents to Promising Antitumor Candidates. Pharmaceuticals 2025, 18, 1813. https://doi.org/10.3390/ph18121813

AMA Style

Simionescu N, Al-Matarneh A, Mangalagiu II, Cibotariu N, Uritu CM, Al-Matarneh CM, Pinteala M. Reinvestigating Pyrrol-2-One-Based Compounds: From Antimicrobial Agents to Promising Antitumor Candidates. Pharmaceuticals. 2025; 18(12):1813. https://doi.org/10.3390/ph18121813

Chicago/Turabian Style

Simionescu, Natalia, Ashraf Al-Matarneh, Ionel I. Mangalagiu, Narcis Cibotariu, Cristina Mariana Uritu, Cristina Maria Al-Matarneh, and Mariana Pinteala. 2025. "Reinvestigating Pyrrol-2-One-Based Compounds: From Antimicrobial Agents to Promising Antitumor Candidates" Pharmaceuticals 18, no. 12: 1813. https://doi.org/10.3390/ph18121813

APA Style

Simionescu, N., Al-Matarneh, A., Mangalagiu, I. I., Cibotariu, N., Uritu, C. M., Al-Matarneh, C. M., & Pinteala, M. (2025). Reinvestigating Pyrrol-2-One-Based Compounds: From Antimicrobial Agents to Promising Antitumor Candidates. Pharmaceuticals, 18(12), 1813. https://doi.org/10.3390/ph18121813

Note that from the first issue of 2016, this journal uses article numbers instead of page numbers. See further details here.

Article Metrics

Article metric data becomes available approximately 24 hours after publication online.
Back to TopTop