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Bioorg Med Chem Lett. 2016 Dec 15;26(24):5860-5862. doi: 10.1016/j.bmcl.2016.11.020. Epub 2016 Nov 12.

3-Cyano-6-(5-methyl-3-pyrazoloamino) pyridines (Part 2): A dual inhibitor of Aurora kinase and tubulin polymerization.

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R&D, Marketing & Business Planning Division, CXS Corporation, 22 Yamashita-cho, Naka-ku, Yokohama 231-0023, Japan. Electronic address:


A new class of a dual inhibitor of Aurora kinase and tubulin polymerization was created by introducing various substituted phenoxyethylamino or pyridyloxyethylamino groups to the 2-position of 3-cyano-4-methyl-6-(5-methyl-3-pyrazoloamino)-pyridine. Compound 3g exhibited Aurora kinase inhibition, excellent protein kinase selectivity to Aurora kinase in comparison with 66 other kinases, inhibition of phosphorylation of Ser10 of histone H3 as an Aurora kinase inhibitor, inhibition of tubulin polymerization in vitro, good cell membrane permeability, and a good PK profile. Therefore compound 3g was effective in some antitumor mouse models at a dose of 30mg/kgpoqd.


Anti-cancer reagent; Aurora kinase inhibitor; Tubulin polymerization inhibitor

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