McGuinness B.F.,Ligand Pharmaceuticals Inc. |
Ho K.-K.,Ligand Pharmaceuticals Inc. |
Stauffer T.M.,Ligand Pharmaceuticals Inc. |
Rokosz L.L.,Ligand Pharmaceuticals Inc. |
And 17 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010
A novel series of quinolinone-based adenosine A2B 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 A2B antagonist (2i) which exhibited potent activity in a cAMP accumulation assay (5.1 nM) and an IL-8 release assay (0.4 nM). © 2010 Elsevier Ltd. All rights reserved.