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Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068. Epub 2014 Apr 29.

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.

Author information

1
Array BioPharma Inc, Boulder, CO 80301, USA. Electronic address: jblake@arraybiopharma.com.
2
Array BioPharma Inc, Boulder, CO 80301, USA.
3
Genentech Inc, 1 DNA Way, South San Francisco, CA 94080-4990, USA.

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.

KEYWORDS:

Erk2 kinase inhibitors; Mek resistance; Structure based drug design

PMID:
24813737
DOI:
10.1016/j.bmcl.2014.04.068
[Indexed for MEDLINE]

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