| Literature DB >> 21055932 |
Brian F McGuinness1, Koc-Kan Ho, Tara M Stauffer, Laura L Rokosz, Neelima Mannava, Steven G Kultgen, Kurt Saionz, Anthony Klon, Weiqing Chen, Hema Desai, W Lynn Rogers, Maria Webb, Juxing Yin, Yan Jiang, Tailong Li, Hao Yan, Konghua Jing, Shengting Zhang, Kanak Kanti Majumdar, Vikash Srivastava, Samiran Saha.
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).Entities:
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Year: 2010 PMID： 21055932 DOI： 10.1016/j.bmcl.2010.10.030
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823