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Bioorg Med Chem Lett
; 24(12): 2635-9, 2014 Jun 15.
Article
in English
| MEDLINE
| ID: mdl-24813737
ABSTRACT
The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts.