874382-49-7Relevant academic research and scientific papers
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)
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.
Pyrazolopyrimidine piperazinone compounds as well as preparation method and application thereof
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, (2020/09/21)
The invention provides a pyrazolopyrimidine piperazinone compound as well as a preparation method and application thereof, and belongs to the field of organic compound synthesis and medical application. The structural formula of the pyrazolopyrimidine piperazinone compound is shown in the specification. Tests prove that the pyrazolopyrimidine piperazinone compound provided by the invention has strong inhibitory activity on Akt1 kinase, has anti-proliferative activity on mantle cell lymphoma (MCL) and has good practical application value.
