The preparation and SAR of 4-(anilino), 4-(phenoxy), and 4-(thiophenoxy)-quinazolines: inhibitors of p56 lck and EGF-R tyrosine kinase activity

…, CYJ Hsu, A Zilberstein, SE Johnson, LE Hook…

Index: Myers, Michael R.; Setzer, Natalie N.; Spada, Alfred P.; Zulli, Allison L.; Hsu, Chin-Yi J.; Zilberstein, Asher; Johnson, Susan E.; Hook, Linda E.; Jacoski, Mary V. Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 4 p. 417 - 420

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Citation Number: 68

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.