THE PREPARATION AND SAR OF 4-(ANILINO), 4-(PHENOXY), AND 4-(THIOPHENOXY)-QUINAZOLINES - INHIBITORS OF P56(LCK) AND EGF-R TYROSINE KINASE-ACTIVITY

Authors
MYERS MR SETZER NN SPADA AP ZULLI AL HSU CYJ ZILBERSTEIN A JOHNSON SE HOOK LE JACOSKI MV
Citation
Mr. Myers et al., THE PREPARATION AND SAR OF 4-(ANILINO), 4-(PHENOXY), AND 4-(THIOPHENOXY)-QUINAZOLINES - INHIBITORS OF P56(LCK) AND EGF-R TYROSINE KINASE-ACTIVITY, Bioorganic & medicinal chemistry letters, 7(4), 1997, pp. 417-420
Citations number
29
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
4
Year of publication
1997
Pages
417 - 420
Database
ISI
SICI code
0960-894X(1997)7:4<417:TPASO4>2.0.ZU;2-4
Abstract
We report herein our preliminary results of a SAR study of quinazoline -based inhibitors of p56(lck) and EGF-R tyrosine kinase activity.(1) T he most potent inhibitor of p56(lck) identified, RPR-108518A (10), has an IC50 of 0.50 mu M. The 3-chlorophenoxy- and 3-chlorothiophenoxy- d erivatives 5 and 6 were also shown to be extremely potent EGF-R inhibi tors. (C) 1997, Elsevier Science Ltd.