644981-89-5Relevant articles and documents
Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant
Zhang, Daoguang,Tong, Dongdong,Yang, Dezhi,Sun, Jing,Zhang, Fenghe,Zhao, Guisen
, p. 1340 - 1350 (2018/08/28)
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.
Substituted Heterocyclic Ethers and Their Use in CNS Disorders
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Page/Page column 41, (2009/01/24)
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.