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  • Title: Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.
    Author: Cai ZW, Wei D, Schroeder GM, Cornelius LA, Kim K, Chen XT, Schmidt RJ, Williams DK, Tokarski JS, An Y, Sack JS, Manne V, Kamath A, Zhang Y, Marathe P, Hunt JT, Lombardo LJ, Fargnoli J, Borzilleri RM.
    Journal: Bioorg Med Chem Lett; 2008 Jun 01; 18(11):3224-9. PubMed ID: 18479916.
    Abstract:
    A series of acylurea analogs derived from pyrrolopyridine and aminopyridine scaffolds were identified as potent inhibitors of Met kinase activity. The SAR at various positions of the two kinase scaffolds was investigated. These studies led to the discovery of compounds 3b and 20b, which demonstrated favorable pharmacokinetic properties in mice and significant antitumor activity in a human gastric carcinoma xenograft model.
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