| Literature DB >> 20573509 |
Ryoichi Ando1, Hiroshi Ikegami, Makoto Sakiyama, Shinsuke Ooike, Masayuki Hayashi, Yasuhiro Fujino, Daisuke Abe, Hideo Nakamura, Tadashi Mishina, Harutoshi Kato, Yumiko Iwase, Hideo Tomozane, Masahiko Morioka.
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. Copyright 2010. Published by Elsevier Ltd.Entities:
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Year: 2010 PMID： 20573509 DOI： 10.1016/j.bmcl.2010.04.119
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823