Author/Authors :
Christian Zechel، نويسنده , , Gisela Backfisch، نويسنده , , Jürgen Delzer، نويسنده , , Hervé Geneste، نويسنده , , Claudia Graef، نويسنده , , Wilfried Hornberger، نويسنده , , Andreas Kling، نويسنده , , Udo E. W. Lange، نويسنده , , Arnulf Lauterbach، نويسنده , , Werner Seitz، نويسنده , , Thomas Subkowski، نويسنده ,
Abstract :
Solid-phase synthesis and SAR of αVβ3-receptor antagonists based on a N1-substituted 4-amino-1H-pyrimidin-2-one scaffold are described. The most potent compounds exhibited IC50 values towards αVβ3 in the nano- to subnanomolar range and high selectivity versus related integrins like αIIbβ3. For selected examples efficacy in functional cellular assays was demonstrated.
