4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.

Liddle, John; Bamborough, Paul; Barker, Michael D; Campos, Sebastien; Cousins, Rick P C; Cutler, Geoffrey J; Hobbs, Heather; Holmes, Duncan S; Ioannou, Chris; Mellor, Geoff W; Morse, Mary A; Payne, Jeremy J; Pritchard, John M; Smith, Kathryn J; Tape, Daniel T; Whitworth, Caroline; Williamson, Richard A

Liddle, John; Bamborough, Paul; Barker, Michael D; Campos, Sebastien; Cousins, Rick P C; Cutler, Geoffrey J; Hobbs, Heather; Holmes, Duncan S; Ioannou, Chris; Mellor, Geoff W; Morse, Mary A; Payne, Jeremy J; Pritchard, John M; Smith, Kathryn J; Tape, Daniel T; Whitworth, Caroline; Williamson, Richard A.

Affiliation

Liddle J; GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK.

Bioorg Med Chem Lett ; 19(9): 2504-8, 2009 May 01.

Article in En | MEDLINE | ID: mdl-19349179

ABSTRACT

The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.

Subject(s)

Chemistry, Pharmaceutical/methods; I-kappa B Kinase/antagonists & inhibitors; Indoles/chemical synthesis; Indoles/pharmacology; Adenosine Triphosphate/chemistry; Binding Sites; Drug Design; Humans; Inhibitory Concentration 50; Models, Chemical; Models, Molecular; Molecular Structure; Protein Binding; Structure-Activity Relationship; Sulfonamides/chemistry

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Chemistry, Pharmaceutical / I-kappa B Kinase / Indoles Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Document type: Article Country of publication: United kingdom

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