Literature DB >> 15125939

Hit-to-lead studies: the discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors.

Andrew Baxter1, Steve Brough, Anne Cooper, Eike Floettmann, Steve Foster, Christine Harding, Jason Kettle, Tom McInally, Craig Martin, Michelle Mobbs, Maurice Needham, Pete Newham, Stuart Paine, Steve St-Gallay, Sylvia Salter, John Unitt, Yafeng Xue.   

Abstract

A hit-to-lead optimisation programme was carried out on the thiophenecarboxamide high throughput screening hits 1 and 2 resulting in the discovery of the potent and orally bioavailable IKK-2 inhibitor 22.

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Year:  2004        PMID： 15125939     DOI： 10.1016/j.bmcl.2004.03.058

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


  18 in total

1.  Palmitate-induced C/EBP homologous protein activation leads to NF-κB-mediated increase in BACE1 activity and amyloid beta genesis.

Authors:  Gurdeep Marwarha; Jared Schommer; Jonah Lund; Trevor Schommer; Othman Ghribi
Journal:  J Neurochem       Date:  2018-02-14       Impact factor: 5.372

2.  Kaposi's sarcoma-associated herpesvirus-encoded viral FLICE inhibitory protein (vFLIP) K13 suppresses CXCR4 expression by upregulating miR-146a.

Authors:  V Punj; H Matta; S Schamus; A Tamewitz; B Anyang; P M Chaudhary
Journal:  Oncogene       Date:  2009-12-21       Impact factor: 9.867

Review 3.  Inhibitory kappa B Kinases as targets for pharmacological regulation.

Authors:  Carly Gamble; Kathryn McIntosh; Rebecca Scott; Ka Ho Ho; Robin Plevin; Andrew Paul
Journal:  Br J Pharmacol       Date:  2012-02       Impact factor: 8.739

4.  Latent HIV-1 infection occurs in multiple subsets of hematopoietic progenitor cells and is reversed by NF-κB activation.

Authors:  Lucy A McNamara; Janani A Ganesh; Kathleen L Collins
Journal:  J Virol       Date:  2012-06-20       Impact factor: 5.103

5.  3D QSAR pharmacophore model based on diverse IKKβ inhibitors.

Authors:  Shanthi Nagarajan; Asif Ahmed; Hyunah Choo; Yong Seo Cho; Kwang-Seok Oh; Byung Ho Lee; Kye Jung Shin; Ae Nim Pae
Journal:  J Mol Model       Date:  2010-04-25       Impact factor: 1.810

6.  A selective novel low-molecular-weight inhibitor of IkappaB kinase-beta (IKK-beta) prevents pulmonary inflammation and shows broad anti-inflammatory activity.

Authors:  Karl Ziegelbauer; Florian Gantner; Nicholas W Lukacs; Aaron Berlin; Kinji Fuchikami; Toshiro Niki; Katsuya Sakai; Hisayo Inbe; Keisuke Takeshita; Mina Ishimori; Hiroshi Komura; Toshiki Murata; Timothy Lowinger; Kevin B Bacon
Journal:  Br J Pharmacol       Date:  2005-05       Impact factor: 8.739

7.  Integrated microarray and multiplex cytokine analyses of Kaposi's Sarcoma Associated Herpesvirus viral FLICE Inhibitory Protein K13 affected genes and cytokines in human blood vascular endothelial cells.

Authors:  Vasu Punj; Hittu Matta; Sandra Schamus; Preet M Chaudhary
Journal:  BMC Med Genomics       Date:  2009-08-06       Impact factor: 3.063

8.  Evidence for active antigen presentation by monocyte/macrophages in response to stimulation with particles: the expression of NFκB transcription factors and costimulatory molecules.

Authors:  Huwaidha Altaf; Peter A Revell
Journal:  Inflammopharmacology       Date:  2013-05-14       Impact factor: 4.473

9.  Induction of CCL20 production by Kaposi sarcoma-associated herpesvirus: role of viral FLICE inhibitory protein K13-induced NF-kappaB activation.

Authors:  Vasu Punj; Hittu Matta; Sandra Schamus; Tianbing Yang; Yuan Chang; Preet M Chaudhary
Journal:  Blood       Date:  2009-03-26       Impact factor: 22.113

10.  IKKβ inhibitor identification: a multi-filter driven novel scaffold.

Authors:  Shanthi Nagarajan; Hyunah Choo; Yong Seo Cho; Kye Jung Shin; Kwang-Seok Oh; Byung Ho Lee; Ae Nim Pae
Journal:  BMC Bioinformatics       Date:  2010-10-15       Impact factor: 3.169
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