Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2012 Mar 15;22(6):2283-6.
doi: 10.1016/j.bmcl.2012.01.105. Epub 2012 Feb 2.

Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors

Joerg Bussenius  1 , Neel K Anand, Charles M Blazey, Owen J Bowles, Lynne Canne Bannen, Diva S-M Chan, Baili Chen, Erick W Co, Simona Costanzo, Steven C DeFina, Larisa Dubenko, Stefan Engst, Maurizio Franzini, Ping Huang, Vasu Jammalamadaka, Richard G Khoury, Moon H Kim, Rhett R Klein, Douglas Laird, Donna T Le, Morrison B Mac, David J Matthews, David Markby, Nicole Miller, John M Nuss, Jason J Parks, Tsze H Tsang, Amy L Tsuhako, Yong Wang, Wei Xu, Kenneth D Rice
Affiliations

Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors

Joerg Bussenius et al. Bioorg Med Chem Lett. .

Abstract

The 70-kDa ribosomal protein S6 kinase (p70S6K) is part of the PI3K/AKT/mTOR pathway and has been implicated in cancer. High throughput screening versus p70S6K led to the identification of aminopyrimidine 3a as active inhibitor. Lead optimization of 3a resulted in highly potent, selective, and orally bioavailable pyrazolopyrimidines. In this manuscript we report the structure-activity relationship of this series and pharmacokinetic, pharmacodynamic, and efficacy data of the lead compound 13c.

PubMed Disclaimer

MeSH terms

LinkOut - more resources