2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2010 Aug 1;20(15):4709-11. doi: 10.1016/j.bmcl.2010.04.119.
Ryoichi Ando 1,  Hiroshi Ikegami,  Makoto Sakiyama,  Shinsuke Ooike,  Masayuki Hayashi,  Yasuhiro Fujino,  Daisuke Abe,  Hideo Nakamura,  Tadashi Mishina,  Harutoshi Kato,  Yumiko Iwase,  Hideo Tomozane,  Masahiko Morioka
Affiliations

Affiliation

  • 1 Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation, Aoba-ku, Yokohama 227-0033, Japan.
PMID: 20573509 DOI: 10.1016/j.bmcl.2010.04.119
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.

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