Title of article
N-Aryl-γ-lactams as integrin αvβ3 antagonists
Author/Authors
Ning Xi، نويسنده , , Stephen Arvedson، نويسنده , , Shawn Eisenberg، نويسنده , , Nianhe Han، نويسنده , , Michael Handley، نويسنده , , Liang Huang، نويسنده , , Qi Huang، نويسنده , , Alexander Kiselyov، نويسنده , , Qingyian Liu، نويسنده , , Yuelie Lu، نويسنده , , Gladys Nunez، نويسنده , , Timothy Osslund، نويسنده , , David Powers، نويسنده , , Andrew S. Tasker، نويسنده , , Ling Wang، نويسنده , , Tingjian Xiang، نويسنده , , Shimin Xu، نويسنده , , Jiandong Zhang، نويسنده , , Jiawang Zhu، نويسنده , , Richard Kendall، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
2905
To page
2909
Abstract
Novel αvβ3 antagonists based on the N-aryl-γ-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for αvβ3 receptor with excellent selectivity against the structurally related αIIbβ3 receptor. Additional interactions of N-aryl-γ-lactam derivatives with αvβ3 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.
Keywords
fax: +1-805-480-1337 , e-mail: celiad@amgen.com , avb3.* Corresponding author. Tel.: +1-805-447-2211 , Integrin antagonists
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794507
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