| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10587308 | Bioorganic & Medicinal Chemistry Letters | 2013 | 28 Pages |
Abstract
A highly ligand efficient, novel 8-oxo-pyridopyrimidine containing inhibitor of Jak1 and Jak2 isoforms with a pyridone moiety as the hinge-binding motif was discovered. Structure-based design strategies were applied to significantly improve enzyme potency and the polarity of the molecule was adjusted to gain cellular activity. The crystal structures of two representative inhibitors bound to Jak1 were obtained to enable SAR exploration.
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Authors
Sharada Labadie, Kathy Barrett, Wade S. Blair, Christine Chang, Gauri Deshmukh, Charles Eigenbrot, Paul Gibbons, Adam Johnson, Jane R. Kenny, Pawan Bir Kohli, Marya Liimatta, Patrick J. Lupardus, Steven Shia, Micah Steffek, Savita Ubhayakar,