Inhibitors of epidermal growth factor receptor tyrosine kinase: Optimisation of potency and in vivo pharmacokinetics

被引：33
作者：
Ballard, Peter
Bradbury, Robert H.
Harris, Craig S.
Hennequin, Laurent F. A.
Hickinson, Mark
Kettle, Jason G.
Kendrew, Jane
Klinowska, Teresa
Ogilvie, Donald J.
Pearson, Stuart E.
Williams, Emma J.
Wilson, Ingrid
机构：
[1] AstraZeneca, Macclesfield SK10 4TG, Cheshire, England
[2] AstraZeneca, Ctr Rech, F-51689 Reims 2, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 18期
关键词：
EGF; kinase; inhibitor; DMPK;
D O I：
10.1016/j.bmcl.2006.06.054
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The structure-activity and structure-property relationships of anilinoquinazoline inhibitors of EGFR were investigated. Strategies to lower volume of distribution and shorten half-life through structure and pK(a) modulation are discussed. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4908 / 4912
页数：5
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