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ID: ALA3758137
Journal: Eur J Med Chem
Title: Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.
Authors: Liu Y, Jin S, Peng X, Lu D, Zeng L, Sun Y, Ai J, Geng M, Hu Y.
Abstract: Over activation of c-Met tyrosine kinase is known to promote tumorigenesis and metastasis, as well as to cause therapeutic resistance. Herein we describe the design, synthesis and biological activities of novel, ATP-competitive, c-Met tyrosine kinase inhibitors that are members of the 6-aryl-2-(3-(heteroarylamino)benzyl)pyridazinone family. A structure-activity relationship (SAR) study of these substances led to identification of pyridazinone 19 as a highly selective and potent c-Met tyrosine inhibitor, which displays favorable pharmacokinetic properties in mice and significant antitumor activity against a c-Met driven EBC-1 tumor xenograft.
CiteXplore: 26698536