Literature DB >> 20060294

Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.

Juraj Velcicky1, Roland Feifel, Stuart Hawtin, Richard Heng, Christine Huppertz, Guido Koch, Markus Kroemer, Henrik Moebitz, Laszlo Revesz, Clemens Scheufler, Achim Schlapbach.   

Abstract

New, selective 3-aminopyrazole based MK2-inhibitors were discovered by scaffold hopping strategy. The new derivatives proved to inhibit intracellular phosphorylation of hsp27 as well as LPS-induced TNFalpha release in cells. In addition, selected derivative 14e also inhibited LPS-induced TNFalpha release in vivo. Copyright (c) 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 20060294     DOI： 10.1016/j.bmcl.2009.10.138

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


  13 in total

1.  The p38 MAP Kinase Family as Regulators of Proinflammatory Cytokine Production in Degenerative Diseases of the CNS.

Authors:  Adam D Bachstetter; Linda J Van Eldik
Journal:  Aging Dis       Date:  2010-09-24       Impact factor: 6.745

Review 2.  Classification of scaffold-hopping approaches.

Authors:  Hongmao Sun; Gregory Tawa; Anders Wallqvist
Journal:  Drug Discov Today       Date:  2011-10-26       Impact factor: 7.851

3.  Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors.

Authors:  Jun Qin; Pawan Dhondi; Xianhai Huang; Robert Aslanian; James Fossetta; Fang Tian; Daniel Lundell; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2011-12-23       Impact factor: 4.345

4.  Structure of the β-form of human MK2 in complex with the non-selective kinase inhibitor TEI-L03090.

Authors:  Aiko Fujino; Kei Fukushima; Takaharu Kubota; Yoshiyuki Matsumoto; Midori Takimoto-Kamimura
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2013-11-28

5.  Modulating ADME Properties by Fluorination: MK2 Inhibitors with Improved Oral Exposure.

Authors:  Juraj Velcicky; Achim Schlapbach; Richard Heng; Laszlo Revesz; Daniel Pflieger; Ernst Blum; Stuart Hawtin; Christine Huppertz; Roland Feifel; Rene Hersperger
Journal:  ACS Med Chem Lett       Date:  2018-03-20       Impact factor: 4.345

Review 6.  Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.

Authors:  Mario Fiore; Stefano Forli; Fabrizio Manetti
Journal:  J Med Chem       Date:  2015-11-09       Impact factor: 7.446

7.  Approaches towards the synthesis of 5-aminopyrazoles.

Authors:  Ranjana Aggarwal; Vinod Kumar; Rajiv Kumar; Shiv P Singh
Journal:  Beilstein J Org Chem       Date:  2011-02-09       Impact factor: 2.883

8.  Binding affinity prediction for ligands and receptors forming tautomers and ionization species: inhibition of mitogen-activated protein kinase-activated protein kinase 2 (MK2).

Authors:  Senthil Natesan; Rajesh Subramaniam; Charles Bergeron; Stefan Balaz
Journal:  J Med Chem       Date:  2012-02-17       Impact factor: 7.446

9.  Microwave-Assisted Synthesis of a MK2 Inhibitor by Suzuki-Miyaura Coupling for Study in Werner Syndrome Cells.

Authors:  Mark C Bagley; Mohammed Baashen; Irina Chuckowree; Jessica E Dwyer; David Kipling; Terence Davis
Journal:  Pharmaceuticals (Basel)       Date:  2015-06-03

10.  A computational study on thiourea analogs as potent MK-2 inhibitors.

Authors:  Ming Hao; Hong Ren; Fang Luo; Shuwei Zhang; Jieshan Qiu; Mingjuan Ji; Hongzong Si; Guohui Li
Journal:  Int J Mol Sci       Date:  2012-06-08       Impact factor: 6.208
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