871339-34-3Relevant articles and documents
Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors
Bussenius, Joerg,Anand, Neel K.,Blazey, Charles M.,Bowles, Owen J.,Bannen, Lynne Canne,Chan, Diva S.-M.,Chen, Baili,Co, Erick W.,Costanzo, Simona,Defina, Steven C.,Dubenko, Larisa,Engst, Stefan,Franzini, Maurizio,Huang, Ping,Jammalamadaka, Vasu,Khoury, Richard G.,Kim, Moon H.,Klein, Rhett R.,Laird, Douglas,Le, Donna T.,Mac, Morrison B.,Matthews, David J.,Markby, David,Miller, Nicole,Nuss, John M.,Parks, Jason J.,Tsang, Tsze H.,Tsuhako, Amy L.,Wang, Yong,Xu, Wei,Rice, Kenneth D.
, p. 2283 - 2286 (2012/05/04)
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.
KINASE MODULATORS AND METHODS OF USE
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, (2010/02/15)
The present invention relates to compounds of the Formula I and II wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.