| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372495 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
A series of (hetero)arylpyrimidines agonists of the Wnt-β-catenin cellular messaging system have been prepared. These compounds show activity in U2OS cells transfected with Wnt-3a, TCF-luciferase, Dkk-1 and tk-Renilla. Selected compounds show minimal GSK-3β inhibition indicating that the Wnt-β-catenin agonism activity most likely comes from interaction at Wnt-3a/Dkk-1. Two examples 1 and 25 show in vivo osteogenic activity in a mouse calvaria model. One example 1 is shown to activate non-phosphorylated β-catenin formation in bone.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Adam M. Gilbert, Matthew G. Bursavich, Nippa Alon, Bheem M. Bhat, Frederick J. Bex, Michael Cain, Valerie Coleburn, Virginia Gironda, Paula Green, Diane B. Hauze, Yogendra Kharode, Girija Krishnamurthy, Matthew Kirisits, Ho-Sun Lam, Yao-Bin Liu,