Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue 4, Pages 1170-1187Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm401805h
Keywords
-
Categories
Ask authors/readers for more resources
Crizotinib (1), an anaplastic. lymphoma kinase (ALK) receptor tyrosine kinase inhibitor approved by the U.S. Food and Drug Administration in 2011, is efficacious in ALK and ROS positive patients. Under pressure of crizotinib treatment, point mutations arise in the kinase domain of ALK, resulting in resistance and progressive disease. The successful application of both structure-based and lipophilic-efficiency-focused drug design resulted in aminopyridine 8e, which was potent across a broad panel of engineered ALK mutant cell lines and showed suitable preclinical pharmacokinetics and robust tumor growth inhibition in a crizotinib-resistant cell line (H3122-L1196M).
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available