| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371935 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3.
Graphical abstractExtensive SAR studies of a series derived from RY-337, a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead, led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3. Analogs in this series demonstrated good rat pharmacokinetics.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Shuwen He, Peter H. Dobbelaar, Jian Liu, Tianying Jian, Iyassu K. Sebhat, Linus S. Lin, Allan Goodman, Cheng Guo, Peter R. Guzzo, Mark Hadden, Alan J. Henderson, Megan Ruenz, Bruce J. Sargent, Larry Yet, Theresa M. Kelly, Oksana Palyha, Yanqing Kan,