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  • 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.

3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.

Bioorganic & medicinal chemistry letters (2010-06-25)
Ryoichi Ando, Hiroshi Ikegami, Makoto Sakiyama, Shinsuke Ooike, Masayuki Hayashi, Yasuhiro Fujino, Daisuke Abe, Hideo Nakamura, Tadashi Mishina, Harutoshi Kato, Yumiko Iwase, Hideo Tomozane, Masahiko Morioka
PMID20573509
ABSTRACT

A new class of Aurora A kinase inhibitor was created by transforming 4-(5-methyl-3-pyrazoloamino)pyrimidine moiety of VX-680 to 3-cyano-6-(5-methyl-3pyrazoloamino)pyridine. Compound 6 exhibited a potent Aurora A kinase inhibitory activity, excellent selectivity to Aurora B kinase and other 60 kinases, good cell permeability and good PK profile. Therefore compound 6 was effective in antitumor mice model at a dose of 30 mg/kg po qd without decrease of body weight.