4836-52-6Relevant articles and documents
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Lintermans,Bearden
, p. 18 (1972)
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Hit to lead studies on (hetero)arylpyrimidines-Agonists of the canonical Wnt-β-catenin cellular messaging system
Gilbert, Adam M.,Bursavich, Matthew G.,Alon, Nippa,Bhat, Bheem M.,Bex, Frederick J.,Cain, Michael,Coleburn, Valerie,Gironda, Virginia,Green, Paula,Hauze, Diane B.,Kharode, Yogendra,Krishnamurthy, Girija,Kirisits, Matthew,Lam, Ho-Sun,Liu, Yao-Bin,Lombardi, Sabrina,Matteo, Jeanne,Murrills, Richard,Robinson, John A.,Selim, Sally,Sharp, Michael,Unwalla, Raymond,Varadarajan, Usha,Zhao, Weiguang,Yaworsky, Paul J.
experimental part, p. 366 - 370 (2010/04/06)
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.