Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2014 May 15;24(10):2278-82. doi: 10.1016/j.bmcl.2014.03.075. Epub 2014 Apr 3.

Syk inhibitors with high potency in presence of blood.

Author information

1
Novartis Institutes for Biomedical Research, Forum 1 Novartis Campus, 4056 Basel, Switzerland. Electronic address: gebhard.thoma@novartis.com.
2
Novartis Institutes for Biomedical Research, Forum 1 Novartis Campus, 4056 Basel, Switzerland.
3
Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.

Abstract

We describe two series of Syk inhibitors which potently abrogate Syk kinase function in enzymatic assays, cellular assays and in primary cells in the presence of blood. Introduction of a 7-aminoindole substituent led to derivatives with good kinase selectivity and little or no hERG channel inhibition (3b, 10c).

KEYWORDS:

Aldehyde oxidase; BIIB-057; Fostamatinib; Kinase inhibitors; Spleen tyrosine kinase

PMID:
24726806
DOI:
10.1016/j.bmcl.2014.03.075
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center