Jump to main content
Jump to site search


Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant

Author affiliations

Abstract

A series of AKT inhibitors possessing a piperidin-4-yl side chain was designed and synthesized. Some of them showed high AKT1 inhibitory activity and potent anti-proliferative effect on PC-3 prostate cancer cells in the preliminary screening. Further studies revealed the most potent compound, 10h, as a pan-AKT inhibitor. Compound 10h was able to inhibit the cellular phosphorylation of AKT effectively and induce apoptosis of PC-3 cells. It also showed high metabolic stability in human liver microsomes. Preclinical characterization of 10h, a promising lead AKT inhibitor, as a potential anti-prostate cancer therapeutic needs to be further investigated.

Graphical abstract: Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant

Back to tab navigation

Publication details

The article was received on 13 Apr 2018, accepted on 28 Jun 2018 and first published on 03 Jul 2018


Article type: Research Article
DOI: 10.1039/C8MD00197A
Citation: Med. Chem. Commun., 2018, Advance Article
  •   Request permissions

    Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant

    D. Zhang, D. Tong, D. Yang, J. Sun, F. Zhang and G. Zhao, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8MD00197A

Search articles by author

Spotlight

Advertisements