Evidence map›Paper›PMID 29472124›Full record

ArticleBioorganic & medicinal chemistry2018

Design, synthesis and biological assessment of N-adamantyl, substituted adamantyl and noradamantyl phthalimidines for nitrite, TNF-α and angiogenesis inhibitory activities.

Weiming Luo, David Tweedie, Shaunna L Beedie, Neil Vargesson, William D Figg, Nigel H Greig, Michael T Scerba

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
1.6field-weighted citation impact, top 19% 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

13 citing papers in PubMed, 18 citations in OpenAlex.

  1. Article
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  5. ACS pharmacology & translational science · 2021
    Article
  6. Review
  7. Article
  8. Article
  9. Article
  10. MiR-130b/TNF-α/NF-κB/VEGFA loop inhibits prostate cancer angiogenesis.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2020
    Article
  11. Article
  12. Article
  13. Review
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

7 authors at 2 institutions in 2 countries.

Weiming LuoDrug Design & Development Section, Translational Gerontology Branch, Intramural Research Program, National Institute on Aging, National Institutes of Health, Baltimore, MD 21224, USA.
David TweedieDrug Design & Development Section, Translational Gerontology Branch, Intramural Research Program, National Institute on Aging, National Institutes of Health, Baltimore, MD 21224, USA.
Shaunna L BeedieSchool of Medicine, Medical Sciences and Nutrition, Institute of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen AB25 2ZD, UK; Molecular Pharmacology Section, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
Neil VargessonSchool of Medicine, Medical Sciences and Nutrition, Institute of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen AB25 2ZD, UK.
William D FiggMolecular Pharmacology Section, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
Nigel H GreigDrug Design & Development Section, Translational Gerontology Branch, Intramural Research Program, National Institute on Aging, National Institutes of Health, Baltimore, MD 21224, USA. Electronic address: greign@grc.nia.nih.gov.
Michael T ScerbaDrug Design & Development Section, Translational Gerontology Branch, Intramural Research Program, National Institute on Aging, National Institutes of Health, Baltimore, MD 21224, USA.
National Institutes of Health · USUniversity of Aberdeen · GB

Funding

Pro-inflammatory cytokine lowering anti-inflammatory drugsZIAAG000994 · NIA · NATIONAL INSTITUTE ON AGING · PI GREIG, NIGEL H. · 2016 to 2025
$16.8M
Development of Anticancer AgentsZIASC006538 · NCI · DIVISION OF CLINICAL SCIENCES - NCI · PI FIGG, WILLIAM DOUGLAS · 2009 to 2025
$8.6M
ALZHEIMERS RESEARCH PROJECT: Alzheimer's disease drug developmentZIAAG000469 · NIA · NATIONAL INSTITUTE ON AGING · PI GREIG, NIGEL H. · 2019 to 2025
$6.7M
Intramural NIH HHS Z99 AG999999Intramural NIH HHS ZIA AG000994Wellcome TrustWellcome Trust 098252/Z/12/Z
6 · The paper itself

Abstract

A library of 15 novel and heretofore uncharacterized adamantyl and noradamantyl phthalimidines was synthesized and evaluated for neuroprotective and anti-angiogenic properties. Phthalimidine treatment in LPS-challenged cells effected reductions in levels of secreted TNF-α and nitrite relative to basal amounts. The primary SAR suggests nitration of adamantyl phthalimidines has marginal effect on TNF-α activity but promotes anti-nitrite activity; thioamide congeners retain anti-nitrite activity but are less effective reducing TNF-α. Site-specific nitration and thioamidation provided phthalimidine 24, effecting an 88.5% drop in nitrite concurrent with only a 4% drop in TNF-α. Notable anti-angiogenesis activity was observed for 20, 21 and 22.

Indexed as

Drug DesignAngiogenesis InhibitorsAnimalsCells, CulturedCell SurvivalDose-Response Relationship, DrugLipopolysaccharidesMiceMolecular StructureNeuroprotective AgentsNitritesPhthalimidesRAW 264.7 CellsStructure-Activity RelationshipTumor Necrosis Factor-alphaAngiogenesis InhibitorsLipopolysaccharidesNeuroprotective AgentsNitritesPhthalimidesphthalimidineTumor Necrosis Factor-alpha

Identifiers

PMID29472124
PMCPMC5891396
OpenAlexW2790493131

What OpenQuestion holds

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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.