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Bioorg Med Chem Lett. 2010 Dec 15;20(24):7414-20. doi: 10.1016/j.bmcl.2010.10.030. Epub 2010 Nov 4.

Discovery of novel quinolinone adenosine A2B antagonists.

Author information

1
Ligand Pharmaceuticals, 3000 Eastpark Boulevard Cranbury, NJ 08512, USA. bmcguinness@venenumbiodesign.com

Abstract

A novel series of quinolinone-based adenosine A(2B) receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted essential structural features of the initial hit. Optimization resulted in an A(2B) antagonist (2i) which exhibited potent activity in a cAMP accumulation assay (5.1 nM) and an IL-8 release assay (0.4 nM).

PMID:
21055932
DOI:
10.1016/j.bmcl.2010.10.030
[Indexed for MEDLINE]

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