Title of article :
The preparation and sar of 4-(anilino), 4-(phenoxy), and 4-(thiophenoxy)-quinazolines: Inhibitors of p56lck and EGF-R tyrosine kinase activity
Author/Authors :
Michael R. Myers، نويسنده , , Natalie N. Setzer، نويسنده , , Alfred. P. Spada، نويسنده , , Allison L. Zulli، نويسنده , , Chin-Yi J. Hsu، نويسنده , , Asher Zilberstein، نويسنده , , Susan E. Johnson، نويسنده , , Linda E. Hook، نويسنده , , Mary V. Jacoski، نويسنده ,
Abstract :
We report herein our preliminary results of a SAR study of quinazoline-based inhibitors of p56lck and EGF-R tyrosine kinase activity.1 The most potent inhibitor of p56lck identified, RPR-108518A (10), has an IC50 of 0.50 μM. The 3-chlorophenoxy- and 3-chlorothiophenoxy- derivatives 5 and 6 were also shown to be extremely potent EGF-R inhibitors.
