Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374886 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
The SAR and improvement in potency against Tie2 of novel thienopyrimidine and thiazolopyrimidine kinase inhibitors are reported. The crystal structure of one of these compounds bound to the Tie-2 kinase domain is consistent with the SAR. These compounds have moderate potency in cellular assays of Tie-2 inhibition, good physical properties, DMPK, and show evidence of in vivo inhibition of Tie-2.
Graphical abstractThe SAR and improvement in potency against Tie-2 of novel thienopyrimidine and thiazolopyrimidine kinase inhibitors are reported. These compounds have moderate potency in cellular assays of Tie-2 inhibition, good physical properties, DMPK, and show evidence of in vivo inhibition of Tie-2.Figure optionsDownload full-size imageDownload as PowerPoint slide