Quinoline-carboxylic acids are potent inhibitors that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins

被引：19

作者：

Zhu, YF ^{[1
]}

Wang, XC ^{[1
]}

Connors, P ^{[1
]}

Wilcoxen, K ^{[1
]}

Gao, YH ^{[1
]}

Gross, R ^{[1
]}

Strack, N ^{[1
]}

Gross, T ^{[1
]}

McCarthy, JR ^{[1
]}

Xie, Q ^{[1
]}

Ling, N ^{[1
]}

Chen, C ^{[1
]}

机构：

[1] Neurocrine Biosci Inc, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(03)00322-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

4-Benzylquinolines 5, based on a series of isoquinolines 1, were prepared and tested as inhibitors of the IGF/IGFBP-3 complex based on their ability to displace IGF-I from its binding to IGF-binding protein-3. SAR studies on the 6,7-dihydroxy moiety of the quinoline 5a showed that the catecol moiety could be replaced with other functional groups. Computational modeling of the 5a/mini-IGFBP-5 complex revealed the possible binding site of 5a on IGFBP-5. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：1931 / 1934

页数：4

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