Evidence map›Paper›PMID 36179402›Full record

ArticleEuropean journal of medicinal chemistry2022

Alkyl-substituted N-methylaryl-N'-aryl-4-aminobenzamides: A new series of small molecule inhibitors for Wip1 phosphatase.

Marco Robello, Hongchao Zheng, Mrinmoy Saha, Kara M George Rosenker, Subrata Debnath, Jay Prakash Kumar, Harichandra D Tagad, Sharlyn J Mazur, Ettore Appella, Daniel H Appella

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact, top 82% 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

0 citing papers in PubMed, 0 citations in OpenAlex.

No citing paper in PubMed yet.

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

10 authors at 1 institution in 1 country.

Marco RobelloLaboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD, 20892, United States.
Hongchao ZhengLaboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD, 20892, United States.
Mrinmoy SahaLaboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD, 20892, United States.
Kara M George RosenkerLaboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD, 20892, United States.
Subrata DebnathLaboratory of Cell Biology, NCI, National Institutes of Health, Bethesda, MD, 20892, United States.
Jay Prakash KumarLaboratory of Cell Biology, NCI, National Institutes of Health, Bethesda, MD, 20892, United States.
Harichandra D TagadLaboratory of Cell Biology, NCI, National Institutes of Health, Bethesda, MD, 20892, United States.
Sharlyn J MazurLaboratory of Cell Biology, NCI, National Institutes of Health, Bethesda, MD, 20892, United States.
Ettore AppellaLaboratory of Cell Biology, NCI, National Institutes of Health, Bethesda, MD, 20892, United States.
Daniel H AppellaLaboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD, 20892, United States. Electronic address: appellad@niddk.nih.gov.
National Institutes of Health · US

Funding

Chemically Modified Peptide Nucleic AcidsZIADK031143 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI APPELLA, DANIEL H · 2009 to 2025
$13.9M
Small Molecule Activators of p53Z01DK031123 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI APPELLA, DANIEL H · 2005 to 2008
$595k
Intramural NIH HHS Z01 DK031123Intramural NIH HHS ZIA DK031143
6 · The paper itself

Abstract

The wild-type p53 induced phosphatase 1 (Wip1), a member of the serine/threonine-specific PP2C family, is overexpressed in numerous human cancers. Wip1 dephosphorylates p53 as well as several kinases (such as p38 MAPK, ATM, Chk1, and Chk2) in the DNA damage response pathway that are responsible for maintaining genomic stability and preventing oncogenic transformation. As a result, Wip1 is an attractive target for synthetic inhibitors that could be further developed into therapeutics to treat some cancers. In this study, we report a series of alkyl-substituted N-methylaryl-N'-aryl-4-aminobenzamides and their inhibitory activity of the Wip1 phosphatase. A straightforward synthetic route was developed to synthesize the target compounds from commercially available starting materials. Three different portions (R

Indexed as

Phosphoprotein PhosphatasesTumor Suppressor Protein p53BenzamidesDNA DamageHumanspara-AminobenzoatesPhosphorylationProtein Phosphatase 2CProtein Serine-Threonine Kinases4-aminobenzamideBenzamidespara-AminobenzoatesPhosphoprotein PhosphatasesProtein Phosphatase 2CProtein Serine-Threonine KinasesTumor Suppressor Protein p53AminobenzamidesCancer treatmentCross couplingPhosphateSmall molecule inhibitorsWip1 phosphatase

Identifiers

PMID36179402
PMCPMC9664485
OpenAlexW4296222888

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.