Evidence map›Paper›PMID 27540279›Full record

ArticleDrug design, development and therapy2016

NAD(P)H:quinone oxidoreductase 1 inducer activity of some novel anilinoquinazoline derivatives.

Mostafa M Ghorab, Mansour S Alsaid, Maureen Higgins, Albena T Dinkova-Kostova, Abdelaaty A Shahat, Nehal H Elghazawy, Reem K Arafa

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Drug design, development and therapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Article
  2. Fucoxanthin Prevents 6-OHDA-Induced Neurotoxicity by Targeting Keap1.Oxidative medicine and cellular longevity · 2021
    Article
  3. 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

7 authors.

Mostafa M GhorabDepartment of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia; Department of Drug Radiation Research, National Center for Radiation Research & Technology, Atomic Energy Authority, Cairo, Egypt.
Mansour S AlsaidDepartment of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.
Maureen HigginsJacqui Wood Cancer Centre, Division of Cancer Research, Medical Research Institute, University of Dundee, Dundee, UK.
Albena T Dinkova-KostovaJacqui Wood Cancer Centre, Division of Cancer Research, Medical Research Institute, University of Dundee, Dundee, UK; Department of Medicine; Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, USA.
Abdelaaty A ShahatDepartment of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia; Phytochemistry Department, National Research Center, Dokki, Giza.
Nehal H ElghazawyZewail City of Science and Technology.
Reem K ArafaZewail City of Science and Technology; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Funding

Cancer Research UK 10270Cancer Research UK 18644
6 · The paper itself

Abstract

The Kelch-like ECH-associated protein 1 (Keap1)/nuclear factor erythroid 2-related factor 2 (Nrf2)/antioxidant response elements pathway enables cells to survive oxidative stress conditions through regulating the expression of cytoprotective enzymes such as NAD(P)H: quinone oxidoreductase 1 (NQO1). This work presents the design and synthesis of novel anilinoquinazoline derivatives (2-16a) and evaluation of their NQO1 inducer activity in murine cells. Molecular docking of the new compounds was performed to assess their ability to inhibit Keap1-Nrf2 protein-protein interaction through occupying the Keap1-Nrf2-binding domain, which leads to Nrf2 accumulation and enhanced gene expression of NQO1. Docking results showed that all compounds can potentially interact with Keap1; however, 1,5-dimethyl-2-phenyl-4-(2-phenylquinazolin-4-ylamino)-1,2-dihydropyrazol-3-one (9), the most potent inducer, showed the largest number of interactions with key amino acids in the binding pocket (Arg483, Tyr525, and Phe478) compared to the native ligand or any other compound in this series.

Indexed as

AnimalsCell Line, TumorDose-Response Relationship, DrugKelch-Like ECH-Associated Protein 1MiceModels, MolecularMolecular StructureNADNAD(P)H Dehydrogenase (Quinone)NF-E2-Related Factor 2Protein BindingQuinazolinesStructure-Activity RelationshipKeap1 protein, mouseKelch-Like ECH-Associated Protein 1NADNAD(P)H Dehydrogenase (Quinone)Nfe2l2 protein, mouseNF-E2-Related Factor 2Nqo1 protein, mouseQuinazolinescytoprotectionKeap1/Nrf2Kelch domainmolecular modelingNQO1 induction

Identifiers

PMID27540279
PMCPMC4982500

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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.