Author(s): Hodous BL, GeunsMeyer SD, Hughes PE, Albrecht BK, Bellon S,
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Abstract A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and KDR selectivity could be achieved with 3-substituted terminal aryl rings. X-ray co-crystal structure analysis aided inhibitor design. This series was evaluated on the basis of potency, selectivity, and rat pharmacokinetic parameters.
This article was published in Bioorg Med Chem Lett
and referenced in Medicinal Chemistry