Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 9, Pages 510-515Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml100178g
Keywords
Insulin-like growth factor-1 receptor (IGF-1R); insulin receptor (IR); inhibitors; structure-based drug design (SBDD); cancer
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This report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). Structure-activity relationship exploration and optimization leading to the identification, characterization, and pharmacological activity of compound 9b, a potent, selective, well-tolerated, and orally bioavailable dual inhibitor of IGF-1R and IR with in vivo efficacy in tumor xenograft models, is discussed.
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