Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6788-92. doi: 10.1016/j.bmcl.2009.09.080. Epub 2009 Sep 25.

2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors.

Author information

1
Ligand Pharmaceuticals, Inc, Cranbury, NJ 08512, USA. acole@ligand.com

Abstract

A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2-benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent of the purinone, compound 24 was identified incorporating a chroman-based functional group. Compound 24 shows excellent kinase activity, good oral bioavailability and demonstrates efficacy in an acute mechanistic mouse model through inhibition of interleukin-2 (IL-2) induced interferon-gamma (INF-gamma) production.

PMID:
19836234
DOI:
10.1016/j.bmcl.2009.09.080
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center