Evidence map›Paper›PMID 21831638›Full record

ArticleBioorganic & medicinal chemistry letters2011

Sulfonamides as a new scaffold for hypoxia inducible factor pathway inhibitors.

Chalet Tan, Rita G de Noronha, Narra S Devi, Adnan A Jabbar, Stefan Kaluz, Yuan Liu, Suazette Reid Mooring, K C Nicolaou, Binghe Wang, Erwin G Van Meir

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing 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

18 citing papers in PubMed.

  1. Article
  2. Review
  3. Arylsulfonamide 64B Inhibits Hypoxia/HIF-Induced Expression of c-Met and CXCR4 and Reduces Primary Tumor Growth and Metastasis of Uveal Melanoma.Clinical cancer research : an official journal of the American Association for Cancer Research · 2019
    Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. Review
  10. Review
  11. Small-molecule proteomimetic inhibitors of the HIF-1α-p300 protein-protein interaction.Chembiochem : a European journal of chemical biology · 2014
    Article
  12. Review
  13. Arylsulfonamide KCN1 inhibits in vivo glioma growth and interferes with HIF signaling by disrupting HIF-1α interaction with cofactors p300/CBP.Clinical cancer research : an official journal of the American Association for Cancer Research · 2012
    Article
  14. Article
  15. Article
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  18. 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.

Chalet TanLaboratory of Molecular Neuro-Oncology, Department of Neurosurgery, Emory University School of Medicine, Atlanta, GA, USA.
Rita G de Noronha
Narra S Devi
Adnan A Jabbar
Stefan Kaluz
Yuan Liu
Suazette Reid Mooring
K C Nicolaou
Binghe Wang
Erwin G Van Meir

Funding

Targeting Glioblastoma Using Novel Small Molecule HIF-1 Pathway InhibitorsR01CA116804 · NCI · EMORY UNIVERSITY · PI VAN MEIR, ERWIN G. · 2007 to 2011
$2.5M
TOTAL SYNTHESIS OF CALICHEMICINSR01CA046446 · NCI · UNIVERSITY OF PENNSYLVANIA · PI NICOLAOU, K. C. · 1988 to 1999
–
NCI NIH HHS R01 CA046446NCI NIH HHS R01 CA116804NCI NIH HHS R01CA116804NCI NIH HHS R01CA116804-S1NCI NIH HHS R01CA46446-13
6 · The paper itself

Abstract

Solid tumors generally grow under hypoxic conditions, a pathophysiological change, which activates the expression of genes responsible for malignant, aggressive, and treatment-refractory properties. Hypoxia inducible factor (HIF) is the chief transcription factor regulating hypoxia-driven gene expression. Therefore, the HIF pathway has become a critical target for cancer therapeutics development. We screened a privileged library of about 10,000 natural-product-like compounds using a cell-based assay for HIF-dependent transcriptional activity and identified several arylsulfonamide HIF pathway inhibitors. Among these compounds, the most potent ones showed an IC(50) of ∼0.5 μM in the hypoxia-responsive element (HRE)-luciferase reporter system. Further studies are needed to fully elucidate the mechanism of action of this class of compounds and their structure-activity relationship.

Indexed as

Alkaline PhosphataseCell Line, TumorDose-Response Relationship, DrugHumansHypoxia-Inducible Factor 1Molecular StructureSmall Molecule LibrariesStereoisomerismStructure-Activity RelationshipSulfonamidesTranscription FactorsAlkaline PhosphataseHypoxia-Inducible Factor 1Small Molecule LibrariesSulfonamidesTranscription Factors

Identifiers

PMID21831638
PMCPMC3292863

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.