Synthesis of highly potent and selective hetaryl ureas as integrin αVβ3-Receptor antagonists

Abstract Solid-phase synthesis and SAR of integrin α V β 3 -receptor antagonists containing a urea moiety as non-basic guanidine mimetic are described. The most potent compounds exhibited IC 50 values towards α V β 3 in the nanomolar range and high selectivity versus related integrins like α IIb β 3 . For selected examples efficacy in functional cellular assays is demonstrated.