Literature DB >> 16236504

Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK.

Rudolf Waelchli1, Birgit Bollbuck, Christian Bruns, Thomas Buhl, Jörg Eder, Roland Feifel, Rene Hersperger, Philipp Janser, Laszlo Revesz, Hans-Günter Zerwes, Achim Schlapbach.   

Abstract

The design, synthesis, and the biological evaluation of 2-benzamido-pyrimidines as novel IKK inhibitors are described. By optimization of the lead compound 3, compounds 16 and 24 are identified as good inhibitors of IKK2 with IC(50) values of 40 and 25 nM, respectively. Compound 16 also demonstrated significant in vivo activity in an acute model of cytokine release.

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Year:  2005        PMID： 16236504     DOI： 10.1016/j.bmcl.2005.09.035

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


  62 in total

1.  A novel inhibitor of inducible NOS dimerization protects against cytokine-induced rat beta cell dysfunction.

Authors:  Linlin Zhong; Tuan Tran; Tyler D Baguley; Sang Jun Lee; Adam Henke; Andrew To; Sijia Li; Shan Yu; Fabio A Grieco; Jason Roland; Peter G Schultz; Decio L Eizirik; Nikki Rogers; Arnab K Chartterjee; Matthew S Tremblay; Weijun Shen
Journal:  Br J Pharmacol       Date:  2018-07-14       Impact factor: 8.739

2.  Induced transcription and stability of CELF2 mRNA drives widespread alternative splicing during T-cell signaling.

Authors:  Michael J Mallory; Samuel J Allon; Jinsong Qiu; Matthew R Gazzara; Iulia Tapescu; Nicole M Martinez; Xiang-Dong Fu; Kristen W Lynch
Journal:  Proc Natl Acad Sci U S A       Date:  2015-04-13       Impact factor: 11.205

3.  Inducible RasGEF1B circular RNA is a positive regulator of ICAM-1 in the TLR4/LPS pathway.

Authors:  Wei Lun Ng; Georgi K Marinov; Ee Shan Liau; Yi Lyn Lam; Yat-Yuen Lim; Chee-Kwee Ea
Journal:  RNA Biol       Date:  2016-06-30       Impact factor: 4.652

4.  A naturally derived small molecule NDSM253 inhibits IKK1 to suppress inflammation response and promote bone healing after fracture.

Authors:  Liqi Shen; Yun Xiao; Hui Xie; Hongbin Zhao; Tao Luo; Lin Liu; Xuekun Pan
Journal:  Am J Transl Res       Date:  2021-01-15       Impact factor: 4.060

5.  Proteasome Composition in Cytokine-Treated Neurons and Astrocytes is Determined Mainly by Subunit Displacement.

Authors:  Kara L Shanley; Che-Lin Hu; Oscar A Bizzozero
Journal:  Neurochem Res       Date:  2020-01-14       Impact factor: 3.996

6.  IκB Kinase Inhibitor Attenuates Sepsis-Induced Cardiac Dysfunction in CKD.

Authors:  Jianmin Chen; Julius E Kieswich; Fausto Chiazza; Amie J Moyes; Thomas Gobbetti; Gareth S D Purvis; Daniela C F Salvatori; Nimesh S A Patel; Mauro Perretti; Adrian J Hobbs; Massimo Collino; Muhammad M Yaqoob; Christoph Thiemermann
Journal:  J Am Soc Nephrol       Date:  2016-05-06       Impact factor: 10.121

7.  Differential Effects of Glycyrrhiza Species on Genotoxic Estrogen Metabolism: Licochalcone A Downregulates P450 1B1, whereas Isoliquiritigenin Stimulates It.

Authors:  Tareisha L Dunlap; Shuai Wang; Charlotte Simmler; Shao-Nong Chen; Guido F Pauli; Birgit M Dietz; Judy L Bolton
Journal:  Chem Res Toxicol       Date:  2015-07-16       Impact factor: 3.739

8.  The NF-κB Pathway Promotes Tamoxifen Tolerance and Disease Recurrence in Estrogen Receptor-Positive Breast Cancers.

Authors:  Irida Kastrati; Stacey E P Joosten; Svetlana E Semina; Luis H Alejo; Svitlana D Brovkovych; Joshua D Stender; Hugo M Horlings; Marleen Kok; Elaine T Alarid; Geoffrey L Greene; Sabine C Linn; Wilbert Zwart; Jonna Frasor
Journal:  Mol Cancer Res       Date:  2020-04-03       Impact factor: 5.852

9.  PIM Kinase Inhibitors Block the Growth of Primary T-cell Acute Lymphoblastic Leukemia: Resistance Pathways Identified by Network Modeling Analysis.

Authors:  James T Lim; Neha Singh; Libia A Leuvano; Valerie S Calvert; Emanuel F Petricoin; David T Teachey; Richard B Lock; Megha Padi; Andrew S Kraft; Sathish K R Padi
Journal:  Mol Cancer Ther       Date:  2020-08-04       Impact factor: 6.261

10.  Signaling through hepatocellular A2B adenosine receptors dampens ischemia and reperfusion injury of the liver.

Authors:  Michael A Zimmerman; Almut Grenz; Eunyoung Tak; Maria Kaplan; Douglas Ridyard; Kelley S Brodsky; Mercedes Susan Mandell; Igal Kam; Holger K Eltzschig
Journal:  Proc Natl Acad Sci U S A       Date:  2013-06-28       Impact factor: 11.205
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