Evidence map›Paper›PMID 30626888›Full record

ArticleScientific reports2019

A novel scaffold for EGFR inhibition: Introducing N-(3-(3-phenylureido)quinoxalin-6-yl) acrylamide derivatives.

Daniel Nascimento do Amaral, Jonas Lategahn, Harold Hilarion Fokoue, Eduardo Miguez Bastos da Silva, Carlos Mauricio R Sant'Anna, Daniel Rauh, Eliezer J Barreiro, Stefan Laufer, Lidia Moreira Lima

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2019. 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
5.8field-weighted citation impact, top 3% 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, 50 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Article
  6. Article
  7. Triple targeting of mutant EGFRJournal of enzyme inhibition and medicinal chemistry · 2023
    Article
  8. Article
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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 at 4 institutions in 2 countries.

Daniel Nascimento do AmaralInstituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR; http://www.inct-inofar.ccs.ufrj.br/), Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®, http://www.lassbio.icb.ufrj.br) Universidade Federal do Rio de Janeiro, CCS, Cidade Universitária, Rio de Janeiro, RJ, Brazil.
Jonas LategahnFaculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Straße 4a, D-44227, Dortmund, Germany.ORCID http://orcid.org/0000-0001-5993-7082
Harold Hilarion FokoueInstituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR; http://www.inct-inofar.ccs.ufrj.br/), Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®, http://www.lassbio.icb.ufrj.br) Universidade Federal do Rio de Janeiro, CCS, Cidade Universitária, Rio de Janeiro, RJ, Brazil.ORCID http://orcid.org/0000-0001-7823-127X
Eduardo Miguez Bastos da SilvaInstituto de Macromoléculas (IMA), Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
Carlos Mauricio R Sant'AnnaInstituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR; http://www.inct-inofar.ccs.ufrj.br/), Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®, http://www.lassbio.icb.ufrj.br) Universidade Federal do Rio de Janeiro, CCS, Cidade Universitária, Rio de Janeiro, RJ, Brazil.
Daniel RauhFaculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Straße 4a, D-44227, Dortmund, Germany.
Eliezer J BarreiroInstituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR; http://www.inct-inofar.ccs.ufrj.br/), Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®, http://www.lassbio.icb.ufrj.br) Universidade Federal do Rio de Janeiro, CCS, Cidade Universitária, Rio de Janeiro, RJ, Brazil.
Stefan LauferDepartment of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy and Interfaculty Center for Pharmacogenomics and Drug Research (ICEPHA), Eberhard-Karls-University Tübingen, Auf der Morgenstelle 8, 72076, Tübingen, Germany. stefan.laufer@uni-tuebingen.de.
Lidia Moreira LimaInstituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR; http://www.inct-inofar.ccs.ufrj.br/), Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®, http://www.lassbio.icb.ufrj.br) Universidade Federal do Rio de Janeiro, CCS, Cidade Universitária, Rio de Janeiro, RJ, Brazil. lidialima@icb.ufrj.br.
Universidade Federal do Rio de Janeiro · BRTU Dortmund University · DEUniversidade Federal Rural do Rio de Janeiro · BRUniversity of Tübingen · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Clinical data acquired over the last decade on non-small cell lung cancer (NSCLC) treatment with small molecular weight Epidermal Growth Factor Receptor (EGFR) inhibitors have shown significant influence of EGFR point mutations and in-frame deletions on clinical efficacy. Identification of small molecules capable of inhibiting the clinically relevant EGFR mutant forms is desirable, and novel chemical scaffolds might provide knowledge regarding selectivity among EGFR forms and shed light on new strategies to overcome current clinical limitations. Design, synthesis, docking studies and in vitro evaluation of N-(3-(3-phenylureido)quinoxalin-6-yl) acrylamide derivatives (7a-m) against EGFR mutant forms are described. Compounds 7h and 7l were biochemically active in the nanomolar range against EGFR

Indexed as

AcrylamidesAntineoplastic AgentsProtein Kinase InhibitorsCell Line, TumorDrug DesignErbB ReceptorsHumansMolecular Docking SimulationNeoplasmsAcrylamidesAntineoplastic AgentsEGFR protein, humanErbB ReceptorsProtein Kinase Inhibitors

Identifiers

PMID30626888
PMCPMC6327040
OpenAlexW2909074919

What OpenQuestion holds

Textmetadata
LicenceCC BY
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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.