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  • Title: Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.
    Author: Zhang D, Ai J, Liang Z, Li C, Peng X, Ji Y, Jiang H, Geng M, Luo C, Liu H.
    Journal: Bioorg Med Chem; 2012 Sep 01; 20(17):5169-80. PubMed ID: 22863529.
    Abstract:
    A series of 2-aminopyridine-3-carboxamide derivatives against c-Met were designed and synthesized by employing bioisosteric replacement of heterocyclic moieties with the amide bond. The structure-activity relationship (SAR) at various positions of the scaffold was explored. In this study, a promising compound (S)-24o with a c-Met IC(50) of 0.022 μM was identified. The compound exhibited dose-dependent inhibition of the phosphorylation of c-Met as well as downstream signaling in EBC-1 cells. Furthermore, the interactive binding model of (S)-24o with c-Met was elucidated by virtue of a molecular modeling study.
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