N-Aryl-γ-lactams as integrin αvβ3 antagonists

被引：28
|
作者：
Xi, N
Arvedson, S
Eisenberg, S
Han, NH
Handley, M
Huang, L
Huang, Q
Kiselyov, A
Liu, QY
Lu, YL
Nunez, G
Osslund, T
Powers, D
Tasker, AS
Wang, L
Xiang, TJ
Xu, SM
Zhang, JD
Zhu, JW
Kendall, R
Dominguez, C
机构：
[1] Amgen Inc, Chem Res & Discovery, Thousand Oaks, CA 91320 USA
[2] Amgen Inc, Canc Biol, Thousand Oaks, CA 91320 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 11期
关键词：
integrin antagonists; alpha(v)beta(3);
D O I：
10.1016/j.bmcl.2004.03.033
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel alpha(v)beta(3) antagonists based on the N-aryl-gamma-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for alpha(v)beta(3) receptor with excellent selectivity against the structurally related alpha(IIb)beta(3) receptor. Additional interactions of N-aryl-gamma-lactam derivatives with alpha(v)beta(3) were found when compared to c(-RGDf[NMe]V-) peptide antagonist. The effects of the conformation and configuration of the gamma-lactam core on the binding were also assessed. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2905 / 2909
页数：5
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