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Bioorg Med Chem Lett. 2010 Aug 1;20(15):4709-11. doi: 10.1016/j.bmcl.2010.04.119. Epub 2010 May 25.

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

Author information

1
Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation, Aoba-ku, Yokohama 227-0033, Japan.

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.

PMID:
20573509
DOI:
10.1016/j.bmcl.2010.04.119
[Indexed for MEDLINE]

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