| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369299 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
![Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2](/preview/png/1369299.png "First Page Preview: Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2")
Authors
James F. Blake, John J. Gaudino, Jason De Meese, Peter Mohr, Mark Chicarelli, Hongqi Tian, Rustam Garrey, Allen Thomas, Christopher S. Siedem, Michael B. Welch, Gabrielle Kolakowski, Robert Kaus, Michael Burkard, Matthew Martinson, Huifen Chen,