4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors.
Bioorganic & Medicinal Chemistry Letters(2014)
摘要
Erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2 (EphA2) is an attractive therapeutic target for suppressing tumor progression. In our efforts to discover novel small molecules to inhibit EphA2, a class of compound based on 4-substituted quinazoline containing 7-(morpholin-2-ylmethoxy) group was identified as a novel hit by high throughput screening campaign. Structural modification of parent quinazoline scaffolds by introducing substituents on aniline displayed potent inhibitory activities toward EphA2.
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关键词
Breast cancer,Erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2 (EphA2),Epithelial cell kinase (Eck),Quinazoline
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