Item Details

title

Synthesis and PI 3-Kinase Inhibition Activity of Some Novel 2,4,6-Trisubstituted 1,3,5-Triazines

author

Nelson, R.

author

Schronce, T.

author

Huang, Y.

author

Albugami, A.

author

Kulik, G.

author

Welker, M.

abstract

A number of new trisubstituted triazine phosphatidylinositol 3-kinase (PI3K) inhibitors were prepared via a three-step procedure utilizing sequential nucleophilic aromatic substitution and cross-coupling reactions. All were screened as PI3K inhibitors relative to the well-characterized PI3K inhibitor, ZSTK474. The most active inhibitors prepared here were 2–4 times more potent than ZSTK474. A leucine linker was attached to the most active inhibitor since it would remain on any peptide-containing prodrug after cleavage by a prostate-specific antigen, and it did not prevent inhibition of protein kinase B (Akt) phosphorylation, and hence, the inhibition of PI3K by the modified inhibitor.

subject

triazine synthesis

PI3K inhibitor

prostate cancer

date

2020-03-09T18:02:47Z (accessioned)

2020-03-09T18:02:47Z (available)

7/4/10 (issued)

identifier

Nelson, R., Schronce, T., Huang, Y., Albugami, A., Kulik, G., & Welker, M. (2018). Synthesis and PI 3-kinase inhibition activity of some novel 2, 4, 6-trisubstituted 1, 3, 5-triazines. Molecules, 23(7), 1628. (citation)

http://hdl.handle.net/10339/96047 (uri)

identifier

https://doi.org/10.3390/molecules23071628 (doi)

language

en (iso)

publisher

MDPI

source

Molecules

type

Article