Evidence map›Paper›PMID 28285917›Full record

ArticleBioorganic & medicinal chemistry letters2017

Examining the structure-activity relationship of benzopyran-based inhibitors of the hypoxia inducible factor-1 pathway.

Jalisa Ferguson, Zeus De Los Santos, Narra Devi, Erwin Van Meir, Sarah Zingales, Binghe Wang

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed.

  1. Review
  2. Review
  3. Article
  4. 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
  5. 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

6 authors.

Jalisa FergusonDepartment of Chemistry, Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Zeus De Los SantosDepartment of Chemistry, Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA.
Narra DeviLaboratory of Molecular Neuro-Oncology, Department of Neurosurgery, School of Medicine and Winship Cancer Institute, Emory University, Atlanta, GA 30322, USA.
Erwin Van MeirLaboratory of Molecular Neuro-Oncology, Department of Neurosurgery, School of Medicine and Winship Cancer Institute, Emory University, Atlanta, GA 30322, USA.
Sarah ZingalesDepartment of Chemistry, Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA; Department of Chemistry and Physics, Armstrong State University, Savannah, GA 31419, USA. Electronic address: sarah.zingales@armstrong.edu.
Binghe WangDepartment of Chemistry, Center for Diagnostics and Therapeutics, Georgia State University, Atlanta, GA 30303, USA. Electronic address: wang@gsu.edu.

Funding

Targeting Glioblastoma Using Novel Small Molecule HIF-1 Pathway InhibitorsR01CA116804 · NCI · EMORY UNIVERSITY · PI VAN MEIR, ERWIN G. · 2007 to 2011
$2.5M
Mechanisms of Action for KCN1 in the Control of Uveal Melanoma MetastasisR01CA176001 · NCI · EMORY UNIVERSITY · PI GROSSNIKLAUS, HANS E., VAN MEIR, ERWIN G. · 2014 to 2018
$1.7M
Discovery of chemical probes for uveal melanomaR01CA180805 · NCI · EMORY UNIVERSITY · PI GROSSNIKLAUS, HANS E., VAN MEIR, ERWIN G. · 2013 to 2015
$1.6M
NCI NIH HHS R01 CA116804NCI NIH HHS R01 CA176001NCI NIH HHS R01 CA180805
6 · The paper itself

Abstract

Many forms of solid tumor have a characteristic feature known as hypoxia, which describes a low or non-existent presence of oxygen in the cellular microenvironment. This decrease in oxygen causes activation of the hypoxia inducible factor (HIF) pathway, which activates the transcription of many genes that cause cell proliferation, metastasis, increased glycolysis and angiogenesis. Increased HIF expression has been linked with poor patient prognosis, increased malignancy, and therapeutic resistance. Previous work in our lab has identified 1 and 2 as inhibitors of the HIF pathway, specifically as disrupters of the p300-HIF-1α complex formation. A library of sulfonamide analogs has been designed and synthesized with the intent of examining the SAR of this series of compounds and improving potency and physicochemical properties as compared with lead compounds 1 and 2. At the end, we have achieved a thorough understanding of the structural features critical for future optimization work.

Indexed as

BenzopyransE1A-Associated p300 ProteinHumansHypoxia-Inducible Factor 1, alpha SubunitMolecular Docking SimulationSignal TransductionStructure-Activity RelationshipBenzopyransE1A-Associated p300 ProteinEP300 protein, humanHypoxia-Inducible Factor 1, alpha SubunitHypoxia inducible factor inhibitorsMolecular dockingStructure-activity relationship

Identifiers

PMID28285917
PMCPMC5398316

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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.