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- W2079787008 abstract "Starting from the initial bis-anilinopyrimidine 1, good potency against EphB4 was retained when benzodioxole at C-4 was replaced by an indazole. The key interactions of the indazole with the protein were characterised by crystallographic studies. Further optimisation led to compound 20, a potent inhibitor of the EphB4 and Src kinases with good pharmacokinetics in various preclinical species and high fraction unbound in plasma. Compound 20 may be used as a tool for evaluating the potential of EphB4 kinase inhibitors in vivo." @default.
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- W2079787008 date "2010-11-01" @default.
- W2079787008 modified "2023-10-11" @default.
- W2079787008 title "Inhibitors of the tyrosine kinase EphB4. Part 3: Identification of non-benzodioxole-based kinase inhibitors" @default.
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- W2079787008 doi "https://doi.org/10.1016/j.bmcl.2010.08.100" @default.
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