Evidence map›Paper›PMID 19836860›Full record

ArticleEuropean journal of medicinal chemistry2010

Discovery of colon tumor cell growth inhibitory agents through a combinatorial approach.

Ashraf H Abadi, Dalal A Abouel-Ella, Jochen Lehmann, Heather N Tinsley, Bernard D Gary, Gary A Piazza, Mohammed A O Abdel-Fattah

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
1.8field-weighted citation impact, top 16% 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

15 citing papers in PubMed, 60 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Article
  6. Article
  7. PIM1: a promising target in patients with triple-negative breast cancer.Medical oncology (Northwood, London, England) · 2017
    Review
  8. Article
  9. Article
  10. Article
  11. Article
  12. Article
  13. CoMFA and CoMSIA studies of 1,2-dihydropyridine derivatives as anticancer agents.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2012
    Article
  14. Article
  15. 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 4 institutions in 3 countries.

Ashraf H AbadiDepartment of Parmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo, Cairo 11835, Egypt. ashraf.abadi@guc.edu.eg
Dalal A Abouel-Ella
Jochen Lehmann
Heather N Tinsley
Bernard D Gary
Gary A Piazza
Mohammed A O Abdel-Fattah
Friedrich Schiller University Jena · DEGerman University in Cairo · EGSouthern Research Institute · USUniversity of Alabama at Birmingham · US

Funding

Selective anti-cancer activity of sulindac derivatives on KRAS mutant colon tumor cells by inducing ROSR01CA131378 · NCI · UNIVERSITY OF SOUTH ALABAMA · PI PIAZZA, GARY A · 2008 to 2019
$5.2M
Development of a novel sulindac amide for colorectal cancer chemopreventionR01CA148817 · NCI · UNIVERSITY OF SOUTH ALABAMA · PI PIAZZA, GARY A · 2010 to 2015
$2.4M
Phosphodiesterase 5: A Novel Target and Inhibitor for Breast Cancer ChemopreventionR01CA155638 · NCI · UNIVERSITY OF SOUTH ALABAMA · PI PIAZZA, GARY A · 2012 to 2017
$2.3M
NCI NIH HHS R01 CA131378NCI NIH HHS R01 CA148817NCI NIH HHS R01 CA155638
6 · The paper itself

Abstract

Two series with the general formula of 4,6-diaryl-2-oxo-1,2 dihydropyridine-3-carbonitriles and their isosteric 4,6-diaryl-2-imino-1,2-dihydropyridine-3-carbonitrile were synthesized through one pot reaction of the appropriate acetophenone, aldehyde, ammonium acetate with ethyl cyanoacetate or malononitrile, respectively. The synthesized compounds were evaluated for their tumor cell growth inhibitory activity against the human HT-29 colon tumor cell line, as well as their PDE3 inhibitory activity. Compound 4-(2-Ethoxyphenyl)-2-oxo-6-thiophen-3-yl-1,2-dihydropyridine-3 carbonitrile (21) showed tumor cell growth inhibitory activity with an IC50 value of 1.25 microM. Meanwhile, 4-(4-Ethoxyphenyl)-2-imino-6-(thiophen-3-yl)-1,2-dihydropyridine-3-carbonitrile (26) showed inhibitory effect upon PDE3 using cAMP or cGMP as substrate. No correlation exists between PDE3 inhibition and the tumor cell growth inhibitory activity. Docking compound 21 to other possible molecular targets showed the potential to bind PIM1 Kinase.

Indexed as

Combinatorial Chemistry TechniquesDrug DiscoveryAnimalsAntineoplastic AgentsCell ProliferationColonic NeoplasmsCyclic Nucleotide Phosphodiesterases, Type 3HT29 CellsHumansInhibitory Concentration 50IsoenzymesModels, MolecularMolecular ConformationPhosphodiesterase 3 InhibitorsPyridonesAntineoplastic AgentsCyclic Nucleotide Phosphodiesterases, Type 3IsoenzymesPDE3A protein, humanPhosphodiesterase 3 InhibitorsPyridones

Identifiers

PMID19836860
PMCPMC4980843
OpenAlexW2014980305

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.