Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles

被引：22

作者：

Wissner, A ^{[1
]}

Hamann, PR ^{[1
]}

Nilakantan, R ^{[1
]}

Greenberger, LM ^{[1
]}

Ye, F ^{[1
]}

Rapuano, TA ^{[1
]}

Loganzo, F ^{[1
]}

机构：

[1] Wyeth Ayerst Res, Chem & Screening Sci & Oncol Res, Pearl River, NY 10965 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 06期

关键词：

D O I：

10.1016/j.bmcl.2004.01.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The syntheses and EGFR kinase inhibitory activity of a series of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3carbonitriles are described. Both reversible and irreversible binding inhibitors were prepared. These series were compared with each other and with the corresponding 4-anilinoquinoline-3-carbonitriles. Compounds having a 1,7-naphthyridine core structure can retain high potency while those with a 1,8-naphthyridine core are significantly less active. These results are consistent with molecular modeling observations. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1411 / 1416

页数：6

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