Evidence map›Paper›PMID 33040634›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2020

Design of new disubstituted imidazo[1,2-

Jonathan Elie, Omid Feizbakhsh, Nathalie Desban, Béatrice Josselin, Blandine Baratte, Amandine Bescond, Julien Duez, Xavier Fant, Stéphane Bach, Dominique Marie and 11 more

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
1.7field-weighted citation impact, top 15% 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

9 citing papers in PubMed, 19 citations in OpenAlex.

  1. Article
  2. Article
  3. A ComprehensiveJournal of medicinal chemistry · 2024
    Article
  4. Article
  5. Review
  6. Article
  7. Design and biological evaluation of substituted 5,7-dihydro-6Journal of enzyme inhibition and medicinal chemistry · 2022
    Article
  8. Article
  9. 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

21 authors at 3 institutions in 2 countries.

Jonathan ElieInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Omid FeizbakhshSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Nathalie DesbanSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Béatrice JosselinSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Blandine BaratteSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Amandine BescondSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Julien DuezSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Xavier FantSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Stéphane BachSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Dominique MarieSorbonne Université/CNRS UMR7144, Station Biologique, Roscoff cedex, France.
Matthieu PlaceInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Sami Ben SalahInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Agnes ChartierInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Sabine Berteina-RaboinInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Apirat ChaikuadInstitute for Pharmaceutical Chemistry, Johann Wolfgang Goethe University, Frankfurt am Main, Germany.
Stefan KnappInstitute for Pharmaceutical Chemistry, Johann Wolfgang Goethe University, Frankfurt am Main, Germany.
Fabrice CarlesInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Pascal BonnetInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Frédéric BuronInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Sylvain RoutierInstitut de Chimie Organique et Analytique, Université d'Orléans, UMR CNRS 7311, Orléans Cedex 2, France.
Sandrine RuchaudSorbonne Université/CNRS UMR8227, Station Biologique, Roscoff cedex, France.
Centre National de la Recherche Scientifique · FRUniversité d'Orléans · FRGoethe University Frankfurt · DE

Funding

Wellcome Trust
6 · The paper itself

Abstract

Haspin is a mitotic protein kinase required for proper cell division by modulating Aurora B kinase localisation and activity as well as histone phosphorylation. Here a series of imidazopyridazines based on the CHR-6494 and Structure Activity Relationship was established. An assessment of the inhibitory activity of the lead structures on human Haspin and several other protein kinases is presented. The lead structure was rapidly optimised using a combination of crystal structures and effective docking models, with the best inhibitors exhibiting potent inhibitory activity on Haspin with IC

Indexed as

Amino Acid SequenceAntineoplastic AgentsApoptosisBone NeoplasmsCDC2 Protein KinaseCell Line, TumorCell ProliferationCyclin BDrug Screening Assays, AntitumorHistonesHumansIndazolesIntracellular Signaling Peptides and ProteinsMolecular Docking SimulationOsteosarcomaPhosphorylation3-(1H-indazol-5-yl)-N-propylimidazo(1,2-b)pyridazin-6-amineAntineoplastic AgentsCDC2 Protein KinaseCyclin BHASPIN protein, humanHistonesIndazolesIntracellular Signaling Peptides and ProteinsProtein Kinase InhibitorsProtein Serine-Threonine KinasesPyridazines3D spheroidscellular effectsco-crystallisation and dockingHaspin kinaseImidazopyridazine

Identifiers

PMID33040634
PMCPMC7580722
OpenAlexW3091858640

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.