Evidence mapPaperPMID 39793971Full record

ArticleJournal of medicinal chemistry2025

Novel 3-Sulfonamide Dual-Tail Pyrrol-2-one Bridged Molecules as Potent Human Carbonic Anhydrase Isoform Inhibitors: Design, Synthesis, Molecular Modeling Investigation, and Anticancer Activity in MeWo, SK-BR-3, and MG-63 Cell Lines.

Cristina M Al-Matarneh, Natalia Simionescu, Alina Nicolescu, Mihaela Silion, Andrea Angeli, Niccolò Paoletti, Alessandro Bonardi, Paola Gratteri, Mariana Pinteala, Claudiu T Supuran

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Synthesis and Biological Evaluation ofMolecules (Basel, Switzerland) · 2025
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors.

Cristina M Al-MatarnehCentre of Advanced Research in Bionanoconjugates and Biopolymers, "Petru Poni" Institute of Macromolecular Chemistry of Romanian Academy, 41A Grigore Ghica Voda Alley, Iasi 700487, Romania.ORCID 0000-0001-9299-1347
Natalia SimionescuCentre of Advanced Research in Bionanoconjugates and Biopolymers, "Petru Poni" Institute of Macromolecular Chemistry of Romanian Academy, 41A Grigore Ghica Voda Alley, Iasi 700487, Romania.
Alina NicolescuNMR Laboratory "Petru Poni" Institute of Macromolecular Chemistry of Romanian Academy, 41A Grigore Ghica Voda Alley, Iasi 700487, Romania.
Mihaela SilionPhysics of Polymers and Polymeric Materials Department, "Petru Poni" Institute of Macromolecular Chemistry, 41A Grigore Ghica Voda Alley, Iasi 700487, Romania.
Andrea AngeliSezione di Scienze Farmaceutiche, NeuroFarba Department, Universita degli Studi di Firenze, Via Ugo Schiff 6, Sesto Fiorentino 50019, Italy.ORCID 0000-0002-1470-7192
Niccolò PaolettiNEUROFARBA Department, Pharmaceutical and Nutraceutical Section, Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Florence, Via U. Schiff 6, Sesto Fiorentino 50019, Firenze Italy.ORCID 0000-0002-6874-9419
Alessandro BonardiNEUROFARBA Department, Pharmaceutical and Nutraceutical Section, Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Florence, Via U. Schiff 6, Sesto Fiorentino 50019, Firenze Italy.
Paola GratteriNEUROFARBA Department, Pharmaceutical and Nutraceutical Section, Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Florence, Via U. Schiff 6, Sesto Fiorentino 50019, Firenze Italy.ORCID 0000-0002-9137-2509
Mariana PintealaCentre of Advanced Research in Bionanoconjugates and Biopolymers, "Petru Poni" Institute of Macromolecular Chemistry of Romanian Academy, 41A Grigore Ghica Voda Alley, Iasi 700487, Romania.
Claudiu T SupuranSezione di Scienze Farmaceutiche, NeuroFarba Department, Universita degli Studi di Firenze, Via Ugo Schiff 6, Sesto Fiorentino 50019, Italy.ORCID 0000-0003-4262-0323

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Novel 3-sulfonamide pyrrol-2-one derivatives containing two sulfonamide groups were synthesized via a one-pot, three-component method using trifluoroacetic acid as a catalyst. Structural confirmation was achieved using spectroscopic techniques. The compounds were tested against four selected human carbonic anhydrase isoforms (hCA I, hCA II, hCA IX, and hCA XII). Most derivatives showed significant selectivity for hCA II, with 4h, 4i, 4n, 4k, and 4j demonstrating enhanced activity due to methoxy and hydroxy group patterns. Compound 4o exhibited strong dual selectivity for hCA II and hCA IX, while 4l was the most effective inhibitor of hCA XII. Additionally, 4e showed a preference for hCA XII inhibition. Biological evaluation on MeWo, SK-BR-3, and MG-63 cancer cells showed that compound

Indexed as

Antineoplastic AgentsCarbonic Anhydrase InhibitorsCarbonic AnhydrasesDrug DesignSulfonamidesCell Line, TumorDrug Screening Assays, AntitumorHumansIsoenzymesModels, MolecularMolecular Docking SimulationMolecular StructurePyrrolesStructure-Activity RelationshipAntineoplastic AgentsCarbonic Anhydrase InhibitorsCarbonic AnhydrasesIsoenzymesPyrrolesSulfonamides

Identifiers

PMID39793971
PMCPMC11770631

What Socratic holds

Textmetadata
LicenceCC BY-NC-ND
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.