Synthesis and structure-activity relationships of novel IKK-β inhibitors. Part 2: Improvement of in vitro activity

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 15, 2004, Pages 4013-4017

  Murata, Toshiki ^a   Shimada, Mitsuyuki ^a   Kadono, Hiroshi ^a   Sakakibara, Sachiko ^a   Yoshino, Takashi ^a   Masuda, Tsutomu ^a   Shimazaki, Makoto ^a   Shintani, Takuya ^a   Fuchikami, Kinji ^a   Bacon, Kevin B ^a   Ziegelbauer, Karl B ^a   Lowinger, Timothy B ^a  

^a BAYER YAKUHIN LTD   (Japan)

Author keywords

IKK ; Kinase inhibitor; NF B

Indexed keywords

PYRIDINE DERIVATIVE;

ARTICLE; DRUG ACTIVITY; DRUG POTENCY; ENZYME ACTIVITY; EVALUATION; IC 50; STRUCTURE ACTIVITY RELATION;

ENZYME INHIBITORS; HUMANS; I-KAPPA B KINASE; KINETICS; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PROTEIN-SERINE-THREONINE KINASES; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 3042634221     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.05.040     Document Type: Article

References (8)

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8. 4, filtered, and concentrated under reduced pressure. The residue was purified by column chromatography on silica gel (hexane/ethyl acetate, 2/1) to give a yellow oil, which was then recrystallized from ethanol to give the desired product as a white solid (1.90 g, yield; 34% yield). For further details of the syntheses, see: Murata, T.; Umeda, M.; Sakakibara, S.; Yoshino, T.; Sato, H.; Masuda, T.; Koriyama, Y.; Shimada, M.; Shintani, T.; Kadono, H.; Ziegelbauer, K. B.; Fuchikami, K.; Komura, H.; Lowinger, T. B. WO 0224679, 2002; Chem Abstr. 2002, 136, 279345