Literature DB >> 17659871

Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells.

Mark C Bagley1, Terence Davis, Matthew C Dix, Michal J Rokicki, David Kipling.   

Abstract

The p38 mitogen-activated protein kinase inhibitor VX-745 is prepared rapidly and efficiently in a four-step sequence using a combination of conductive heating and microwave-mediated steps. Its inhibitory activity was confirmed in hTERT immortalized HCA2 and WS dermal fibroblasts at 0.5-1.0 microM concentration by ELISA and immunoblot assay, and displays excellent kinase selectivity over the related stress-activated kinase JNK.

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Year:  2007        PMID: 17659871     DOI: 10.1016/j.bmcl.2007.07.016

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


  6 in total

Review 1.  Diverse roles for MAPK signaling in circadian clocks.

Authors:  Charles S Goldsmith; Deborah Bell-Pedersen
Journal:  Adv Genet       Date:  2013       Impact factor: 1.944

2.  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

Review 3.  Use of p38 MAPK Inhibitors for the Treatment of Werner Syndrome.

Authors:  Mark C Bagley; Terence Davis; Paola G S Murziani; Caroline S Widdowson; David Kipling
Journal:  Pharmaceuticals (Basel)       Date:  2010-06-04

4.  One-pot and efficient synthesis of triazolo[1,2-a]indazole-triones via reaction of arylaldehydes with urazole and dimedone catalyzed by silica nanoparticles prepared from rice husk.

Authors:  Hooshang Hamidian; Samieh Fozooni; Asadollah Hassankhani; Sayed Zia Mohammadi
Journal:  Molecules       Date:  2011-10-26       Impact factor: 4.411

5.  Nijmegen breakage syndrome fibroblasts expressing the C-terminal truncated NBN(p70) protein undergo p38/MK2-dependent premature senescence.

Authors:  Terence Davis; Hannah S E Tivey; Amy J C Brook; David Kipling
Journal:  Biogerontology       Date:  2014-09-12       Impact factor: 4.277

6.  Evaluating the Role of p38 MAPK in the Accelerated Cell Senescence of Werner Syndrome Fibroblasts.

Authors:  Terence Davis; Amy J C Brook; Michal J Rokicki; Mark C Bagley; David Kipling
Journal:  Pharmaceuticals (Basel)       Date:  2016-04-28
  6 in total

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