Bioorganic & medicinal chemistry letters, 2011-12, Vol.21 (23), p.7006-7012
- Watterson, Scott H.
- Langevine, Charles M.
- Van Kirk, Katy
- Kempson, James
- Guo, Junquing
- Spergel, Steven H.
- Das, Jagabandhu
- Moquin, Robert V.
- Dyckman, Alaric J.
- Nirschl, David
- Gregor, Kurt
- Pattoli, Mark A.
- Yang, XiaoXia
- McIntyre, Kim W.
- Yang, Guchen
- Galella, Michael A.
- Booth-Lute, Hollie
- Chen, Laishun
- Yang, Zheng
- Wang-Iverson, David
- McKinnon, Murray
- Dodd, John H.
- Barrish, Joel C.
- Burke, James R.
- Pitts, William J.
2011
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- Autor(en) / Beteiligte
- Watterson, Scott H.
- Langevine, Charles M.
- Van Kirk, Katy
- Kempson, James
- Guo, Junquing
- Spergel, Steven H.
- Das, Jagabandhu
- Moquin, Robert V.
- Dyckman, Alaric J.
- Nirschl, David
- Gregor, Kurt
- Pattoli, Mark A.
- Yang, XiaoXia
- McIntyre, Kim W.
- Yang, Guchen
- Galella, Michael A.
- Booth-Lute, Hollie
- Chen, Laishun
- Yang, Zheng
- Wang-Iverson, David
- McKinnon, Murray
- Dodd, John H.
- Barrish, Joel C.
- Burke, James R.
- Pitts, William J.
- Titel
- Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy- N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5- d]pyrrolo[2,3- b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066)
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2011-12, Vol.21 (23), p.7006-7012
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2011
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- The synthesis, structure–activity relationships (SAR), and biological results of pyridyl-substituted azaindole based tricyclic inhibitors of IKK2 are described. Compound 4m demonstrated potent in vitro potency, acceptable pharmacokinetic and physicochemical properties, and efficacy when dosed orally in a mouse model of inflammatory bowel disease.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2011.09.111Titel-ID: cdi_proquest_miscellaneous_911168121
- Format
- –
- Schlagworte
- Acetamides - chemical synthesis, Acetamides - chemistry, Acetamides - pharmacology, Administration, Oral, animal models, Animals, BMS-066, Drug Discovery, Enzyme Activation - drug effects, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, Heterocyclic Compounds, 3-Ring - chemical synthesis, Heterocyclic Compounds, 3-Ring - chemistry, Heterocyclic Compounds, 3-Ring - pharmacology, Humans, I-kappa B Kinase - antagonists & inhibitors, IKK, IKK2, IKKβ, inflammatory bowel disease, Inflammatory Bowel Diseases - drug therapy, Inhibitory Concentration 50, Mice, Molecular Structure, NF-κB, pharmacokinetics, physicochemical properties, Rats, Structure-Activity Relationship, structure-activity relationships