Highly potent and selective αVβ3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones

Abstract Solid-phase synthesis and SAR of α V β 3 -receptor antagonists based on a N 1 -substituted 4-amino-1H-pyrimidin-2-one scaffold are described. The most potent compounds exhibited IC 50 values towards α V β 3 in the nano- to subnanomolar range and high selectivity versus related integrins like α IIb β 3 . For selected examples efficacy in functional cellular assays was demonstrated.