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Issue 3, 2016
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The effect of RO3201195 and a pyrazolyl ketone P38 MAPK inhibitor library on the proliferation of Werner syndrome cells

Mark C. Bagley,*a  Jessica E. Dwyer,a  Mohammed Baashen,a  Matthew C. Dix,b  Paola G. S. Murziani,b  Michal J. Rokicki,c  David Kiplingc  and  Terence Davis*c 
Author affiliations

* Corresponding authors

a Department of Chemistry, School of Life Sciences, University of Sussex, Falmer, Brighton, East Sussex, UK
E-mail: m.c.bagley@sussex.ac.uk

b School of Chemistry, Main Building, Cardiff University, Park Place, Cardiff, UK

c Institute of Cancer and Genetics, Cardiff University School of Medicine, Heath Park, Cardiff, UK

Abstract

Microwave-assisted synthesis of the pyrazolyl ketone p38 MAPK inhibitor RO3201195 in 7 steps and 15% overall yield, and the comparison of its effect upon the proliferation of Werner Syndrome cells with a library of pyrazolyl ketones, strengthens the evidence that p38 MAPK inhibition plays a critical role in modulating premature cellular senescence in this progeroid syndrome and the reversal of accelerated ageing observed in vitro on treatment with SB203580.

Graphical abstract: The effect of RO3201195 and a pyrazolyl ketone P38 MAPK inhibitor library on the proliferation of Werner syndrome cells

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Publication details

The article was received on 28 Oct 2015, accepted on 11 Nov 2015 and first published on 12 Nov 2015


Article type: Paper
DOI: 10.1039/C5OB02229K
Citation: Org. Biomol. Chem., 2016,14, 947-956
  • Open access: Creative Commons BY license
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    The effect of RO3201195 and a pyrazolyl ketone P38 MAPK inhibitor library on the proliferation of Werner syndrome cells

    M. C. Bagley, J. E. Dwyer, M. Baashen, M. C. Dix, P. G. S. Murziani, M. J. Rokicki, D. Kipling and T. Davis, Org. Biomol. Chem., 2016, 14, 947
    DOI: 10.1039/C5OB02229K

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