Literature DB >> 19376699

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

James Kempson1, Junqing Guo, Jagabandhu Das, Robert V Moquin, Steven H Spergel, Scott H Watterson, Charles M Langevine, Alaric J Dyckman, Mark Pattoli, James R Burke, Xiaoxia Yang, Kathleen M Gillooly, Kim W McIntyre, Laishun Chen, John H Dodd, Murray McKinnon, Joel C Barrish, William J Pitts.   

Abstract

A new series of tricyclic-based inhibitors of IKK have been derived from an earlier lead compound. The synthesis and structure-activity relationships (SAR) are described. Compound 4k inhibited TNF production in rats stimulated with LPS.

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Year:  2009        PMID： 19376699     DOI： 10.1016/j.bmcl.2009.03.159

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  Enantioselective copper-catalyzed alkynylation of benzopyranyl oxocarbenium ions.

Authors:  Harathi D Srinivas; Prantik Maity; Glenn P A Yap; Mary P Watson
Journal:  J Org Chem       Date:  2015-04-07       Impact factor: 4.354

2.  Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.

Authors:  Amy C Hart; Gretchen M Schroeder; Honghe Wan; James Grebinski; Jennifer Inghrim; James Kempson; Junqing Guo; William J Pitts; John S Tokarski; John S Sack; Javed A Khan; Jonathan Lippy; Matthew V Lorenzi; Dan You; Theresa McDevitt; Ragini Vuppugalla; Yueping Zhang; Louis J Lombardo; George L Trainor; Ashok V Purandare
Journal:  ACS Med Chem Lett       Date:  2015-07-10       Impact factor: 4.345

3.  Hit identification of IKKβ natural product inhibitor.

Authors:  Chung-Hang Leung; Daniel Shiu-Hin Chan; Ying-Wei Li; Wang-Fun Fong; Dik-Lung Ma
Journal:  BMC Pharmacol Toxicol       Date:  2013-01-07       Impact factor: 2.483
  3 in total

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