Author/Authors :
Udo E. W. Lange، نويسنده , , Gisela Backfisch، نويسنده , , Jürgen Delzer، نويسنده , , Hervé Geneste، نويسنده , , Claudia Graef، نويسنده , , Wilfried Hornberger، نويسنده , , Andreas Kling، نويسنده , , Arnulf Lauterbach، نويسنده , , Thomas Subkowski، نويسنده , , Christian Zechel، نويسنده ,
Abstract :
Solid-phase synthesis and SAR of integrin αVβ3-receptor antagonists containing a urea moiety as non-basic guanidine mimetic are described. The most potent compounds exhibited IC50 values towards αVβ3 in the nanomolar range and high selectivity versus related integrins like αIIbβ3. For selected examples efficacy in functional cellular assays is demonstrated.
