168618-99-3Relevant articles and documents
Practical synthesis of Vistusertib (AZD2014), an ATP competitive mTOR inhibitor
Shen, Guobing,Liu, Miaoqing,Lu, Jianjun,Meng, Tao
, (2019)
Vistusertib (AZD2014) is a potent, selective inhibitor of mTOR kinase. Prompted by its fascinating biological activity, an efficient and practical synthesis of Vistusertib has been developed from 3-acetylbenzoic acid through six steps in 48% overall yield
Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases
Enkvist, Erki,Kriisa, Marie,Roben, Mart,Kadak, Grete,Raidaru, Gerda,Uri, Asko
scheme or table, p. 6098 - 6101 (2010/06/16)
Previously reported structural fragments that associate with the ATP-binding pocket of basophilic protein kinases were conjugated with d-arginine-containing peptides. Inhibitory potency of the resulting bisubstrate-analog inhibitors towards PKA and ROCK-II extended to subnanomolar range. The conjugates incorporating 2-pyrimidyl-5-amidothiophene fragment had the highest activity and at 100 nM concentration exhibited over 80% inhibition of most of the tested basophilic kinases of the AGC group.
SPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
-
, (2008/12/06)
The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating mammals suffering from the condition of being overweight.
