Author/Authors :
Toshiki Murata، نويسنده , , Mitsuyuki Shimada، نويسنده , , Hiroshi Kadono، نويسنده , , Sachiko Sakakibara، نويسنده , , Takashi Yoshino ، نويسنده , , Tsutomu Masuda، نويسنده , , Makoto Shimazaki، نويسنده , , Takuya Shintani، نويسنده , , Kinji Fuchikami، نويسنده , , Kevin B. Bacon، نويسنده , , Karl B. Ziegelbauer، نويسنده , , Timothy B. Lowinger، نويسنده ,
Abstract :
A series of 2-amino-3-cyano-4-alkyl-6-(2-hydroxyphenyl)pyridine derivatives was synthesized and evaluated as IκB kinase β (IKK-β) inhibitors. Substitution of an aminoalkyl group for the aromatic group at the 4-position on the core pyridine ring resulted in a marked increase in both kinase enzyme and cellular potencies, and provided potent IKK-β inhibitors with IC50 values of below 100 nM.
Keywords :
NF-jB , Kinase inhibitor.* Corresponding author. Tel.: +81-774-75-2483 , IKK-b , e-mail: muratato@kcn.ne.jp , fax: +81-774-75-2510
