1259392-35-2Relevant articles and documents
Discovery of novel quinolinone adenosine A2B antagonists
McGuinness, Brian F.,Ho, Koc-Kan,Stauffer, Tara M.,Rokosz, Laura L.,Mannava, Neelima,Kultgen, Steven G.,Saionz, Kurt,Klon, Anthony,Chen, Weiqing,Desai, Hema,Rogers, W. Lynn,Webb, Maria,Yin, Juxing,Jiang, Yan,Li, Tailong,Yan, Hao,Jing, Konghua,Zhang, Shengting,Majumdar, Kanak Kanti,Srivastava, Vikash,Saha, Samiran
scheme or table, p. 7414 - 7420 (2011/02/23)
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).
