Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1363669 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
High throughput screening of the corporate compound collection led to the identification of a novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2′,3′:4,5]thieno[2,3-b]pyridine derivatives as selective PR agonists. Initial SAR exploration leading to potent and selective agonists 9 and 11, X-ray crystal structure of 9 bound to PR-LBD and preliminary developability data are described.
Graphical abstractA novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2′,3′:4,5]thieno[2,3-b]pyridine derivatives was identified as selective PR agonists. Initial SAR exploration, X-ray crystal structure of 9 bound to PR-LBD, and some preliminary developability data are described.Figure optionsDownload full-size imageDownload as PowerPoint slide