Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent

被引：37

作者：

Myers, MR ^{[1
]}

He, W ^{[1
]}

Hanney, B ^{[1
]}

Setzer, N ^{[1
]}

Maguire, MP ^{[1
]}

Zulli, A ^{[1
]}

Bilder, G ^{[1
]}

Galzcinski, H ^{[1
]}

Amin, D ^{[1
]}

Needle, S ^{[1
]}

Spada, AP ^{[1
]}

机构：

[1] Aventis Pharmaceut, Bridgewater, NJ 08807 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(03)00654-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel substituted 2-anilino- and 2-cycloalkylaminoquinoxalines have been found to be useful and selective inhibitors of PDGF-R autophosphorylation. Replacement of an anilino-substituent with substituted cyclohexylamino- or norbornylamino substituents led to significant improvements in the pharmacokinetic profile of these analogues. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3091 / 3095

页数：5

共 16 条

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