Bioorganic and Medicinal Chemistry Letters p. 417 - 420 (1997)
Update date:2022-08-11
Topics:
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.
We report herein our preliminary results of a SAR study of quinazoline-based inhibitors of p56(lck) and EGF-R tyrosine kinase activity. The most potent inhibitor of p56(lck) 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.
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