N-Aryl-γ-lactams as integrin α_vβ₃ antagonists

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• 作者：Xi ; Ning ; Arvedson ; Stephen ; Eisenberg ; Shawn ; Han ; Nianhe ; Handley ; Michael ; Huang ; Liang ; Huang ; Qi ; et. al.
• 关键词：Integrin antagonists ; α ; _vβ ; ₃
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2004
• 出版时间：June 7, 2004
• 年：2004
• 卷：14
• 期：11
• 页码：2905-2909
• 全文大小：290 K

文摘

Novel α_vβ₃ antagonists based on the N-aryl-γ-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for α_vβ₃ receptor with excellent selectivity against the structurally related α_IIbβ₃ receptor. Additional interactions of N-aryl-γ-lactam derivatives with α_vβ₃ were found when compared to c(-RGDf[NMe]V-) peptide antagonist. The effects of the conformation and configuration of the γ-lactam core on the binding were also assessed.