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

Authors
Cockerill, S Stubberfield, C Stables, J Carter, M Guntrip, S Smith, K McKeown, S Shaw, R Topley, P Thomsen, L Affleck, K Jowett, A Hayes, D Willson, M Woollard, P Spalding, D
Citation
S. Cockerill et al., Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2, BIOORG MED, 11(11), 2001, pp. 1401-1405
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
11
Year of publication
2001
Pages
1401 - 1405
Database
ISI
SICI code
0960-894X(20010604)11:11<1401:IQAPAI>2.0.ZU;2-Q
Abstract
Described herein is the design and synthesis of indazolylaminopyridopyrimid ines 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-dimet hylpyrido[3,4-d]pyrimidine-4,6-diamine 3B. This compound inhibited EGFr and c-erbB-2 enzymes selectively over other kinases. It inhibited the prolifer ation of a range of tumour cell lines in vitro and the growth of BT474 xeno grafts in SCID mice. (C) 2001 Elsevier Science Ltd. All rights reserved.