Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2

被引：72

作者：

Cockerill, S ^{[1
]}

Stubberfield, C ^{[1
]}

Stables, J ^{[1
]}

Carter, M ^{[1
]}

Guntrip, S ^{[1
]}

Smith, K ^{[1
]}

McKeown, S ^{[1
]}

Shaw, R ^{[1
]}

Topley, P ^{[1
]}

Thomsen, L ^{[1
]}

Affleck, K ^{[1
]}

Jowett, A ^{[1
]}

Hayes, D ^{[1
]}

Willson, M ^{[1
]}

Woollard, P ^{[1
]}

Spalding, D ^{[1
]}

机构：

[1] Glaxo Wellcome Res & Ctr, Res Biomet, Enzyme Pharmacol, Oncol Unit,Enzyme Chem 1, Stevenage SG1 2NY, Herts, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(01)00219-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Described herein is the design and synthesis of indazolylaminopyridopyrimidines and quinazolines as inhibitors of the class 1 tyrosine kinase receptor family. Data is presented for N-4-(1-benzyl-1H-indazol-5-yl)-N-6,N-6-dimethylpyrido[3,4-d]pyrimidine-4,6-diamine 3B. This compound inhibited EGFr and c-erbB-2 enzymes selectively over other kinases. It inhibited the proliferation of a range of tumour cell lines in vitro and the growth of BT474 xenografts in SCID mice. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1401 / 1405

页数：5

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