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Molecules 2018, 23(7), 1628; https://doi.org/10.3390/molecules23071628

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

1
Department of Chemistry, Wake Forest University, Winston-Salem, NC 27109, USA
2
Department of Cancer Biology and Comprehensive Cancer Center, Wake Forest School of Medicine, Medical Center Blvd., Winston-Salem, NC 27157, USA
3
Life Sciences program, College of Science, Alfaisal University, Riyadh 11533, Saudi Arabia
*
Authors to whom correspondence should be addressed.
Received: 14 June 2018 / Revised: 30 June 2018 / Accepted: 2 July 2018 / Published: 4 July 2018
(This article belongs to the Section Organic Chemistry)
Full-Text   |   PDF [1130 KB, uploaded 4 July 2018]   |  

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. View Full-Text
Keywords: triazine synthesis; PI3K inhibitor; prostate cancer triazine synthesis; PI3K inhibitor; prostate cancer
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Nelson, R.A., Jr.; Schronce, T.; Huang, Y.; Albugami, A.; Kulik, G.; Welker, M.E. Synthesis and PI 3-Kinase Inhibition Activity of Some Novel 2,4,6-Trisubstituted 1,3,5-Triazines. Molecules 2018, 23, 1628.

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