Evidence map›Paper›PMID 34923887›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2022

2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights.

Mostafa M Elbadawi, Wagdy M Eldehna, Amer Ali Abd El-Hafeez, Warda R Somaa, Amgad Albohy, Sara T Al-Rashood, Keli K Agama, Eslam B Elkaeed, Pradipta Ghosh, Yves Pommier and 1 more

Erratum issuedAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing 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

13 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Review
  6. Design, synthesis,RSC advances · 2025
    Article
  7. Article
  8. Article
  9. Review
  10. Identification of 2-(Frontiers in chemistry · 2024
    Article
  11. Article
  12. Article
  13. The Development of FAK Inhibitors: A Five-Year Update.International journal of molecular sciences · 2022
    Review
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

11 authors.

Mostafa M ElbadawiDepartment of Chemistry, Graduate School of Science, Hiroshima University, Hiroshima, Japan.
Wagdy M EldehnaDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh, Egypt.
Amer Ali Abd El-HafeezPharmacology and Experimental Oncology Unit, Cancer Biology Department, National Cancer Institute, Cairo University, Cairo, Egypt.
Warda R SomaaFaculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh, Egypt.
Amgad AlbohyDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt (BUE), Cairo, Egypt.
Sara T Al-RashoodDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Keli K AgamaDevelopmental Therapeutics Branch, Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD, USA.
Eslam B ElkaeedDepartment of Pharmaceutical Sciences, College of Pharmacy, AlMaarefa University, Riyadh, Saudi Arabia.
Pradipta GhoshDepartment of Cellular and Molecular Medicine, University of California San Diego, La Jolla, CA, USA.
Yves PommierDevelopmental Therapeutics Branch, Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD, USA.
Manabu AbeDepartment of Chemistry, Graduate School of Science, Hiroshima University, Hiroshima, Japan.

Funding

DNA Repair, Cell Cycle Checkpoints and Apoptosis as Targets for Anticancer DrugsZIABC006150 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 2009 to 2025
$23.0M
UCSD Cancer Center Training Program in Drug DevelopmentT32CA121938 · NCI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI Michael Bouvet, Dwayne G. Stupack · 2006 to 2026
$10.3M
Spatial Regulation of RGS and G Protein SignalingR01CA100768 · NCI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI GHOSH, PRADIPTA · 2003 to 2019
$7.4M
Development Therapeutics Branch Clinical TrialsZIABC011746 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 2017 to 2025
$2.6M
Integrators of Metastatic PotentialR01CA238042 · NCI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI GHOSH, PRADIPTA, LUKER, GARY D · 2019 to 2023
$2.3M
Modulation of G proteins by Growth FactorsR01CA160911 · NCI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI GHOSH, PRADIPTA · 2013 to 2017
$1.8M
DNA TOPOISOMERASES AS TARGET OF ACTION OF ANTICANCER DRUGSZ01BC006161 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 1996 to 2008
$1.5M
Intramural NIH HHS Z01 BC006161NCI NIH HHS R01 CA100768NCI NIH HHS R01 CA160911NCI NIH HHS R01 CA238042NCI NIH HHS T32 CA121938
6 · The paper itself

Abstract

In this study, different assortments of 2-arylquinolines and 2,6-diarylquinolines have been developed. Recently, we have developed a new series of 6,7-dimethoxy-4-alkoxy-2-arylquinolines as Topoisomerase I (TOP1) inhibitors with potent anticancer activity. Utilising the SAR outputs from this study, we tried to enhance anticancer and TOP1 inhibitory activities. Though target quinolines demonstrated potent antiproliferative effect, specifically against colorectal cancer DLD-1 and HCT-116, they showed weak TOP1 inhibition which may be attributable to their non-coplanarity. Thereafter, screening against kinase panel revealed their dual inhibitory activity against EGFR and FAK. Quinolines

Indexed as

Antineoplastic AgentsApoptosisCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorErbB ReceptorsFocal Adhesion Kinase 1HumansModels, MolecularMolecular StructureProtein Kinase InhibitorsQuinolinesStructure-Activity RelationshipTumor Cells, CulturedAntineoplastic AgentsEGFR protein, humanErbB ReceptorsFocal Adhesion Kinase 1Protein Kinase InhibitorsPTK2 protein, humanQuinolinesanticancerEGFR inhibitorsFAK inhibitorsmolecular dynamicsQuinoline

Identifiers

PMID34923887
PMCPMC8725837

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.