Literature DB >> 21087862

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.

Alaric J Dyckman1, Charles M Langevine, Claude Quesnelle, James Kempson, Junqing Guo, Patrice Gill, Steven H Spergel, Scott H Watterson, Tianle Li, David S Nirschl, Kathleen M Gillooly, Mark A Pattoli, Kim W McIntyre, Laishun Chen, Murray McKinnon, John H Dodd, Joel C Barrish, James R Burke, William J Pitts.   

Abstract

The synthesis, structure-activity relationships (SAR) and biological evaluation of thiazole based tricyclic inhibitors of IKK2 are described. Compound 9 was determined to be orally efficacious in a murine model of rheumatoid arthritis.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21087862     DOI： 10.1016/j.bmcl.2010.10.133

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


  2 in total

1.  Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.

Authors:  R Moslin; D Gardner; J Santella; Y Zhang; J V Duncia; C Liu; J Lin; J S Tokarski; J Strnad; D Pedicord; J Chen; Y Blat; A Zupa-Fernandez; L Cheng; H Sun; C Chaudhry; C Huang; C D'Arienzo; J S Sack; J K Muckelbauer; C Chang; J Tredup; D Xie; N Aranibar; J R Burke; P H Carter; D S Weinstein
Journal:  Medchemcomm       Date:  2016-12-15       Impact factor: 3.597

2.  Improving the Thermostability and Activity of Transaminase From Aspergillus terreus by Charge-Charge Interaction.

Authors:  Jia-Ren Cao; Fang-Fang Fan; Chang-Jiang Lv; Hong-Peng Wang; Ye Li; Sheng Hu; Wei-Rui Zhao; Hai-Bin Chen; Jun Huang; Le-He Mei
Journal:  Front Chem       Date:  2021-04-14       Impact factor: 5.221
  2 in total

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