Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4)

K Lafleur, D Huang, T Zhou, A Caflisch…

文献索引：Journal of Medicinal Chemistry, , vol. 52, # 20 p. 6433 - 6446

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被引用次数: 67

摘要

... Journal of Medicinal ... Here, we present a medicinal chemistry campaign aimed at improving the affinity of the micromolar hits 3 and 4 identified by in silico ... Chemical synthesis of about 30 derivatives of 3 and 4 yielded six nanomolar inhibitors, one of which (compound 66) has an ...