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Synthesis and PI3 Kinase Inhibition Activity of Some Novel Trisubstituted Morpholinopyrimidines

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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.
subject
triazine synthesis
PI3K inhibitor
prostate cancer
contributor
Wright, E. (author)
Nelson, R. (author)
date
2020-03-09T18:28:33Z (accessioned)
2020-03-09T18:28:33Z (available)
7/10/18 (issued)
identifier
Synthesis and PI3 Kinase Inhibition Activity of Some Novel Trisubstituted Morpholinopyrimidines. Emily W. Wright, Ronald A. Nelson, Jr., Yelena Karpova, George Kulik and Mark E. Welker, Molecules 2018, 23(7), 1675; (citation)
https://doi.org/10.3390/molecules23071675 (doi)
http://hdl.handle.net/10339/96050 (uri)
language
en (iso)
publisher
MDPI
rights
https://creativecommons.org/licenses/by/4.0/ (uri)
source
Molecules
title
Synthesis and PI3 Kinase Inhibition Activity of Some Novel Trisubstituted Morpholinopyrimidines
type
Article

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