Literature DB >> 22182499

Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.

Ashwin U Rao1, Dong Xiao, Xianhai Huang, Wei Zhou, James Fossetta, Dan Lundell, Fang Tian, Prashant Trivedi, Robert Aslanian, Anandan Palani.   

Abstract

Facile synthesis of two new series of tetracyclic azepine and oxazocine analogs is described. These analogs were evaluated for their potential as MAPKAP-K2 (MK2) inhibitors and several were found to be potent at inhibiting MK2 with a non-ATP competitive binding mode. Published by Elsevier Ltd.

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Year:  2011        PMID： 22182499     DOI： 10.1016/j.bmcl.2011.11.113

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


  4 in total

1.  A reversible gene-targeting strategy identifies synthetic lethal interactions between MK2 and p53 in the DNA damage response in vivo.

Authors:  Sandra Morandell; H Christian Reinhardt; Ian G Cannell; Jacob S Kim; Daniela M Ruf; Tanya Mitra; Anthony D Couvillon; Tyler Jacks; Michael B Yaffe
Journal:  Cell Rep       Date:  2013-11-14       Impact factor: 9.423

Review 2.  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

3.  Three-Component Azidation of Styrene-Type Double Bonds: Light-Switchable Behavior of a Copper Photoredox Catalyst.

Authors:  Gabriele Fumagalli; Pauline T G Rabet; Scott Boyd; Michael F Greaney
Journal:  Angew Chem Int Ed Engl       Date:  2015-06-26       Impact factor: 15.336

Review 4.  MAPKAPK2: the master regulator of RNA-binding proteins modulates transcript stability and tumor progression.

Authors:  Sourabh Soni; Prince Anand; Yogendra S Padwad
Journal:  J Exp Clin Cancer Res       Date:  2019-03-08
  4 in total

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