- Synthesis and structure-activity relationships of novel IKK-β inhibitors. Part 2: Improvement of in vitro activity
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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 i
- Murata, Toshiki,Shimada, Mitsuyuki,Kadono, Hiroshi,Sakakibara, Sachiko,Yoshino, Takashi,Masuda, Tsutomu,Shimazaki, Makoto,Shintani, Takuya,Fuchikami, Kinji,Bacon, Kevin B.,Ziegelbauer, Karl B.,Lowinger, Timothy B.
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p. 4013 - 4017
(2007/10/03)
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- Synthesis and structure-activity relationships of novel IKK-β inhibitors. Part 3: Orally active anti-inflammatory agents
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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. Modification of a novel IKK-β inhibitor 1 (IKK-β IC 50=1500nM, Cell IC50=8000nM) at the 4-p
- Murata, Toshiki,Shimada, Mitsuyuki,Sakakibara, Sachiko,Yoshino, Takashi,Masuda, Tsutomu,Shintani, Takuya,Sato, Hiroki,Koriyama, Yuji,Fukushima, Keiko,Nunami, Noriko,Yamauchi, Megumi,Fuchikami, Kinji,Komura, Hiroshi,Watanabe, Akihiko,Ziegelbauer, Karl B.,Bacon, Kevin B.,Lowinger, Timothy B.
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p. 4019 - 4022
(2007/10/03)
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- Pyridine derivatives
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Pyridine compounds of general formula: wherein —R1represents in which R11is hydrogen, C1-6alkyl, halogen, hydroxy, C1-12alkoxy, nitro, amino, C1-6alkylsulfonylamino, C1-6alkoxycarbonyl, C1-6alkylamino, di(C1-6alkyl)amino, C1-6alkanoylamino, phenyl C1-6alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2represents hydrogen or halogen; R3represents hydrogen, —CR31R32R33, or —NR34R35; R4is hydrogen, carbamoyl, CN, carboxyl, etc.; R5is amino, C1-6alkylamino, di C1-6alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
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