Evidence map›Paper›PMID 25025991›Full record

ArticleJournal of medicinal chemistry2014

New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.

Giuseppe La Regina, Ruoli Bai, Antonio Coluccia, Valeria Famiglini, Sveva Pelliccia, Sara Passacantilli, Carmela Mazzoccoli, Vitalba Ruggieri, Lorenza Sisinni, Alessio Bolognesi and 15 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing papers in PubMed
3.7field-weighted citation impact, top 6% of its field
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

25 citing papers in PubMed, 91 citations in OpenAlex.

  1. Article
  2. (Pharmaceuticals (Basel, Switzerland) · 2025
    Article
  3. Article
  4. 4-(3-Phenyl-4-(3,4,5-trimethoxybenzoyl)-1Journal of medicinal chemistry · 2023
    Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. Article
  10. Review
  11. Article
  12. Article
  13. Review
  14. Article
  15. Article
  16. Synthesis of Pyrrolo[3,4-Molecules (Basel, Switzerland) · 2019
    Article
  17. Article
  18. Article
  19. Article
  20. 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

25 authors at 9 institutions in 4 countries.

Giuseppe La ReginaIstituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma , Piazzale Aldo Moro 5, I-00185 Roma, Italy.
Ruoli Bai
Antonio Coluccia
Valeria Famiglini
Sveva Pelliccia
Sara Passacantilli
Carmela Mazzoccoli
Vitalba Ruggieri
Lorenza Sisinni
Alessio Bolognesi
Whilelmina Maria Rensen
Andrea Miele
Marianna Nalli
Romina Alfonsi
Lucia Di Marcotullio
Alberto Gulino
Andrea Brancale
Ettore Novellino
Giulio Dondio
Stefania Vultaggio
Mario Varasi
Ciro Mercurio
Ernest Hamel
Patrizia Lavia
Romano Silvestri
Sapienza University of Rome · ITIstituti di Ricovero e Cura a Carattere Scientifico · ITNational Research Council · ITEuropean Institute of Oncology · ITNational Institutes of Health · USUniversity of Naples Federico II · ITCardiff University · GBInstitute of Molecular Biology and Pathology · ITPharmac · NZ

Funding

Intramural NIH HHS Z99 CA999999
6 · The paper itself

Abstract

We synthesized 3-aroyl-1-arylpyrrole (ARAP) derivatives as potential anticancer agents having different substituents at the pendant 1-phenyl ring. Both the 1-phenyl ring and 3-(3,4,5-trimethoxyphenyl)carbonyl moieties were mandatory to achieve potent inhibition of tubulin polymerization, binding of colchicine to tubulin, and cancer cell growth. ARAP 22 showed strong inhibition of the P-glycoprotein-overexpressing NCI-ADR-RES and Messa/Dx5MDR cell lines. Compounds 22 and 27 suppressed in vitro the Hedgehog signaling pathway, strongly reducing luciferase activity in SAG treated NIH3T3 Shh-Light II cells, and inhibited the growth of medulloblastoma D283 cells at nanomolar concentrations. ARAPs 22 and 27 represent a new potent class of tubulin polymerization and cancer cell growth inhibitors with the potential to inhibit the Hedgehog signaling pathway.

Indexed as

Aniline CompoundsAnimalsAntineoplastic AgentsCell DeathCell Line, TumorCell Membrane PermeabilityCell ProliferationCell SurvivalColchicineDrug Screening Assays, AntitumorGuanidinesHedgehog ProteinsHumansMiceMolecular Docking SimulationM Phase Cell Cycle Checkpoints1-(3-(3-(3,4,5-trimethoxybenzoyl)-1H-pyrrol-1-yl)phenyl)guanidine(1-(3-aminophenyl)-1H-pyrrol-3-yl)(3,4,5-trimethoxyphenyl)methanoneAniline CompoundsAntineoplastic AgentsColchicineGuanidinesHedgehog ProteinsPyrrolesTubulinTubulin Modulators

Identifiers

PMID25025991
PMCPMC4154712
OpenAlexW2016930511

What OpenQuestion holds

Textmetadata
LicenceTDM
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 OpenQuestion graph.