218451-34-4Relevant 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.
A nitrogen-containing heterocyclic phenyl piperidine compound and its preparation method and application
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Paragraph 0065-0068; 0069, (2017/09/01)
The invention discloses a nitrogen-containing heterocyclic phenyl piperidine compound or pharmaceutical salt thereof. The general structural formula a of the compound is as shown in specification, wherein R represents hydrogen, mono-substituted or poly-substituted halogen, methyl, methoxyl, tertiary butyl or trifluoromethyl; and R2 is hydrogen, chlorine, bromine, methyl or ethyl. The compound disclosed by the invention is novel in structure; and by introducing the active amino in the form of a piperidine ring, the configuration of the side-chain amino is reinforced and the rigidity of the compound is enhanced. Through the design transformation, the Akt1 kinase inhibitory activity and the PC-3 cell line growth inhibitory activity of the compound are significantly enhanced.
TRIAZOLOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0548; 0551; 0552; 0553; 0554, (2017/12/28)
Provided are triazolopyridine compounds that are inhibitors of JAK kinase, such as JAK1, compositions containing these compounds and methods for treating diseases mediated by a JAK kinase. In particular, provided are compounds of formula (I), stereoisomer