Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2012 Jul 15;22(14):4645-9. doi: 10.1016/j.bmcl.2012.05.114. Epub 2012 Jun 6.

Structure-based optimization of aminopyridines as PKCθ inhibitors.

Author information

1
Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd, 88 Milton Park, Abingdon OX14 4RY, United Kingdom. juan-miguel_jimenez@vrtx.com

Abstract

The identification of a novel series of PKCθ inhibitors and subsequent optimization using docking based on a crystal structure of PKCθ is described. SAR was rapidly generated around an amino pyridine-ketone hit; (6-aminopyridin-2-yl)(2-aminopyridin-3-yl)methanone 2 leading to compound 21 which significantly inhibits production of IL-2 in a mouse SEB-IL2 model.

PMID:
22738630
DOI:
10.1016/j.bmcl.2012.05.114
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center