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2004
Pyridine derivatives
R 0380
Synthesis and Structure—Activity Relationships of Novel IKK-β Inhibitors. Part
2. Improvement of in vitro Activity. — A series of 4-substituted 2-amino-3-cyano49- 126 -6-(hydroxyphenyl)pyridine
derivatives [cf. (V), (VIII)] are synthesized and evaluated
for their IκB kinase β inhibitory activity. The optimized piperidine analogue (VIIIa)
exhibits not only selective and potent inhibition of IKK-β kinase but also reasonably
potent activity in a variety of relevant cellular assays. — (MURATA*, T.; et al.;
Bioorg. Med. Chem. Lett. 14 (2004) 15, 4013-4017; Dep. Chem., Res. Cent. Kyoto,
Bayer Yakuhin, Ltd., Soraku, Kyoto 619-02, Japan; Eng.) — M. Schroeter
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