Evidence map›Paper›PMID 29996482›Full record

ArticleMolecules (Basel, Switzerland)2018

Synthesis and PI3 Kinase Inhibition Activity of Some Novel Trisubstituted Morpholinopyrimidines.

Emily W Wright, Ronald A Nelson, Yelena Karpova, George Kulik, Mark E Welker

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.1field-weighted citation impact, top 52% 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

1 citing paper in PubMed, 5 citations in OpenAlex.

  1. 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

5 authors at 1 institution in 2 countries.

Emily W WrightDepartment of Chemistry, Wake Forest University, P.O. Box 7486, Winston-Salem, NC 27109, USA. wrighter11@gmail.com.
Ronald A NelsonDepartment of Chemistry, Wake Forest University, P.O. Box 7486, Winston-Salem, NC 27109, USA. rnelson@wakehealth.edu.
Yelena KarpovaDepartment of Cancer Biology and Comprehensive Cancer Center, Wake Forest School of Medicine, Medical Center Blvd., Winston-Salem, NC 27157, USA. ykarpova@wakehealth.edu.
George KulikDepartment of Cancer Biology and Comprehensive Cancer Center, Wake Forest School of Medicine, Medical Center Blvd., Winston-Salem, NC 27157, USA. gkulik@wakehealth.edu.
Mark E WelkerDepartment of Chemistry, Wake Forest University, P.O. Box 7486, Winston-Salem, NC 27109, USA. welker@wfu.edu.
Wake Forest University · US

Funding

A novel mechanism of AKT activation regulated by YY1 bindingR21CA182248 · NCI · WAKE FOREST UNIVERSITY HEALTH SCIENCES · PI KULIK, GEORGE A · 2015 to 2016
$371k
NCI NIH HHS R21 CA182248
6 · The paper itself

Abstract

A number of new substituted morpholinopyrimidines were prepared utilizing sequential nucleophilic aromatic substitution and cross-coupling reactions. One of the disubstituted pyrimidines was converted into two trisubstituted compounds which were screened as PI3K inhibitors relative to the well-characterized PI3K inhibitor ZSTK474, and were found to be 1.5⁻3-times more potent. A leucine linker was attached to the most active inhibitor since it would remain on any peptide-containing prodrug after cleavage by prostate-specific antigen, and it did not prevent inhibition of AKT phosphorylation and hence the inhibition of PI3K by the modified inhibitor.

Indexed as

Phosphoinositide-3 Kinase InhibitorsCell Line, TumorHumansIsomerismLeucinePeptidesPhosphatidylinositol 3-KinasesPhosphorylationProtein Kinase InhibitorsPyrimidinesLeucinePeptidesPhosphatidylinositol 3-KinasesPhosphoinositide-3 Kinase InhibitorsProtein Kinase InhibitorsPyrimidinesPI3K inhibitorprostate cancertriazine synthesis

Identifiers

PMID29996482
PMCPMC6100461
OpenAlexW2833085473

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.