Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase

被引：22

作者：

Ballard, Peter

Barlaam, Bernard C.

Bradbury, Robert H.

Dishington, Allan

Hennequin, Laurent F. A.

Hickinson, D. Mark

Hollingsworth, Ian M.

Kettle, Jason G.

Klinowska, Teresa

Ogilvie, Donald J.

Pearson, Stuart E.

Scott, James S.

Suleman, Abid

Whittaker, Robin

Williams, Emma J.

Wood, Robin

Wright, Lindsay

机构：

[1] AstraZeneca, Canc Infect Res, Macclesfield SK10 4TG, Cheshire, England

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 22期

关键词：

anilinoquinazoline; erbB2-selective inhibitor; tumor growth; cytochrome p450 inhibitor;

D O I：

10.1016/j.bmcl.2007.08.073

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Neutral 5-substituted 4-anilinoquinazolines addressed high in vivo clearance and phospholipidosis associated with previous basic compounds. A representative compound 8a inhibited tumor growth in a mouse xenograft model when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole (ABT), and data are consistent with pharmacology primarily reflecting inhibition of erbB2 receptor tyrosine kinase. (C) 2007 Elsevier Ltd. All rights reserved.

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页码：6326 / 6329

页数：4

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