Synthesis of highly potent and selective hetaryl ureas as integrin α V β 3-Receptor antagonists

…, A Kling, A Lauterbach, T Subkowski, C Zechel

文献索引：Lange, Udo E.W.; Backfisch, Gisela; Delzer, Juergen; Geneste, Herve; Graef, Claudia; Hornberger, Wilfried; Kling, Andreas; Lauterbach, Arnulf; Subkowski, Thomas; Zechel, Christian Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 10 p. 1379 - 1382

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被引用次数: 21

摘要

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.