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Synthesis of highly potent and selective hetaryl ureas as integrin alpha(V)beta3-receptor antagonists
Udo E W Lange1, Gisela Backfisch, Jürgen Delzer
1BASF AG, D-67056, Ludwigshafen, Germany. udo.lange@basf-ag.de
Bioorganic & Medicinal Chemistry Letters
|May 7, 2002
Abstract:
Solid-phase synthesis and SAR of integrin alpha(V)beta3-receptor antagonists containing a urea moiety as non-basic guanidine mimetic are described. The most potent compounds exhibited IC(50) values towards alpha(V)beta3 in the nanomolar range and high selectivity versus related integrins like alpha(IIb)beta3. For selected examples efficacy in functional cellular assays is demonstrated.