Evidence map›Paper›PMID 28523727›Full record

ArticleChemMedChem2017

Synthesis and Antineoplastic Evaluation of Mitochondrial Complex II (Succinate Dehydrogenase) Inhibitors Derived from Atpenin A5.

Hezhen Wang, Bader Huwaimel, Kshitij Verma, James Miller, Todd M Germain, Nihar Kinarivala, Dimitri Pappas, Paul S Brookes, Paul C Trippier

Abstract read
In one paragraph

Article in ChemMedChem, 2017. 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
–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

25 citing papers in PubMed.

  1. Article
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  5. Review
  6. Article
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  15. Article
  16. Synthesis andRoyal Society open science · 2020
    Article
  17. Review
  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

9 authors.

Hezhen WangDepartment of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, School of Pharmacy, Amarillo, TX, 79106, USA.
Bader HuwaimelDepartment of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, School of Pharmacy, Amarillo, TX, 79106, USA.
Kshitij VermaDepartment of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, School of Pharmacy, Amarillo, TX, 79106, USA.
James MillerDepartment of Anesthesiology, University of Rochester Medical Center, Rochester, NY, 14642, USA.
Todd M GermainDepartment of Chemistry and Biochemistry, Texas Tech University, Lubbock, TX, 79409, USA.
Nihar KinarivalaDepartment of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, School of Pharmacy, Amarillo, TX, 79106, USA.
Dimitri PappasDepartment of Chemistry and Biochemistry, Texas Tech University, Lubbock, TX, 79409, USA.
Paul S BrookesDepartment of Anesthesiology, University of Rochester Medical Center, Rochester, NY, 14642, USA.
Paul C TrippierDepartment of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, School of Pharmacy, Amarillo, TX, 79106, USA.ORCID 0000-0002-4947-5782

Funding

SIRT1, Nitro-Lipids and CardioprotectionR01HL071158 · NHLBI · UNIVERSITY OF ROCHESTER · PI BROOKES, PAUL S · 2003 to 2025
$7.7M
NHLBI NIH HHS R01 HL071158
6 · The paper itself

Abstract

Mitochondrial complex II (CII) is an emerging target for numerous human diseases. Sixteen analogues of the CII inhibitor natural product atpenin A5 were prepared to evaluate the structure-activity relationship of the C5 pyridine side chain. The side chain ketone moiety was determined to be pharmacophoric, engendering a bioactive conformation. One analogue, 1-(2,4-dihydroxy-5,6-dimethoxypyridin-3-yl)hexan-1-one (16 c), was found to have a CII IC

Indexed as

AnimalsAntineoplastic AgentsBenzamidesCatalytic DomainCell Line, TumorElectron TransportEtoposideHEK293 CellsHumansMiceModels, MolecularNitrilesPhenylthiohydantoinPyridonesQuantitative Structure-Activity RelationshipSuccinate DehydrogenaseAntineoplastic Agentsatpenin A5BenzamidesenzalutamideEtoposideNitrilesPhenylthiohydantoinPyridonesSuccinate Dehydrogenaseanticancer agentsatpenin A5mitochondriamitochondrial complex IIsuccinate dehydrogenase

Identifiers

PMID28523727
PMCPMC5557372

What OpenQuestion holds

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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.