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

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

  • Bioorg Med Chem Lett. 2007 Sep 15;17(18):5107-10. doi: 10.1016/j.bmcl.2007.07.016.
Mark C Bagley 1,  Terence Davis,  Matthew C Dix,  Michal J Rokicki,  David Kipling
Affiliations

Affiliation

  • 1 School of Chemistry, Main Building, Cardiff University, Park Place, Cardiff CF10 3AT, UK. [email protected]
PMID: 17659871 DOI: 10.1016/j.bmcl.2007.07.016
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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