168618-99-3Relevant academic research and scientific papers
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
PROCESS OF SYNTHESIZING SUBSTITUTED PYRIDINE AND PYRIMIDINE COMPOUND
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, (2018/04/13)
Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II′, wherein the definition of each of groups is as described as the
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.
Synthesis, SAR study and biological evaluation of novel pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as anti-proliferative agents
Wang, Yanong D.,Honores, Erick,Wu, Biqi,Johnson, Steve,Powell, Dennis,Miranda, Miriam,McGinnis, John P.,Discafani, Carolyn,Rabindran, Sridhar K.,Cheng, Wendy,Krishnamurthy, Girija
experimental part, p. 2091 - 2100 (2009/06/06)
Checkpoint deficiency of malignant cells can be exploited in cancer drug discovery. Compounds that selectively kill checkpoint-deficient cells versus checkpoint-proficient cells can be utilized to preferentially target tumor cells, while sparing normal ce
SPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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, (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.
Substituted pyrazolo[1,5-a] pyrimidines and process for making same
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Page/Page column 54, (2010/10/20)
This invention relates to novel pyrazolo[1,5-a]pyrimidine compounds and the therapeutically acceptable salts thereof. These compounds are useful as anti-proliferative agents in mammals, including humans.
