Dowling, James E.; Alimzhanov, Marat; Bao, Larry; Block, Michael H.; Chuaqui, Claudio; Cooke, Emma L.; Denz, Christopher R.; Hird, Alex; Huang, Shan; Larsen, Nicholas A.; Peng, Bo; Pontz, Timothy W.; Rivard-Costa, Caroline; Saeh, Jamal Carlos; Thakur, Kumar; Ye, Qing; Zhang, Tao; Lyne, Paul D. published their research in ACS Medicinal Chemistry Letters on August 8 ,2013. The article was titled 《Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo》.Reference of 2-(3-Amino-1H-pyrazol-1-yl)ethanol The article contains the following contents:
In this letter, we describe the design, synthesis, and structure-activity relationship of 5-anilinopyrazolo[1,5-a]pyrimidine inhibitors, e.g., I, of CK2 kinase. Property-based optimization of early leads using the 7-oxetan-3-yl amino group led to a series of matched mol. pairs with lower lipophilicity, decreased affinity for human plasma proteins, and reduced binding to the hERG ion channel. Agents in this study were shown to modulate pAKTS129, a direct substrate of CK2, in vitro and in vivo, and exhibited tumor growth inhibition when administered orally in a murine DLD-1 xenograft. In the experiment, the researchers used 2-(3-Amino-1H-pyrazol-1-yl)ethanol(cas: 84407-13-6Reference of 2-(3-Amino-1H-pyrazol-1-yl)ethanol)
2-(3-Amino-1H-pyrazol-1-yl)ethanol(cas: 84407-13-6) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Reference of 2-(3-Amino-1H-pyrazol-1-yl)ethanol
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics