Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket

被引：38

作者：

Ballard, P

Bradbury, RH

Harris, CS

Hennequin, LFA

Hickinson, M

Johnson, PD

Kettle, JG

Klinowska, T

Leach, AG

Morgentin, R

Pass, M

Ogilvie, DJ

Olivier, A

Warin, N

Williams, EJ

机构：

[1] AstraZeneca, Macclesfield SK10 4TG, Cheshire, England

[2] AstraZeneca, Ctr Rech, ZI Pompelle, F-51689 Reims 2, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 06期

关键词：

EGF; kinase; inhibitor; quinazoline;

D O I：

10.1016/j.bmcl.2005.12.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel C-5 substituted anilinoquinazolines, selected on the basis of docking experiments and overlays with ATP in the active site of EGFR tyrosine kinase, have been prepared and found to be potent inhibitors. In vivo pharmacokinetics and disease model activity are discussed. (C) 2005 Elsevier Ltd. All rights reserved.

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页码：1633 / 1637

页数：5

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