2. Academic Validation
  3. Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells

Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells

  • Bioorg Med Chem Lett. 2008 Jul 1;18(13):3745-8. doi: 10.1016/j.bmcl.2008.05.037.
Mark C Bagley 1,  Terence Davis,  Matthew C Dix,  Paola G S Murziani,  Michal J Rokicki,  David Kipling
Affiliations

Affiliation

  • 1 School of Chemistry, Main Building, Cardiff University, Park Place, Cardiff CF10 3AT, UK. [email protected]
PMID: 18539026 DOI: 10.1016/j.bmcl.2008.05.037
Abstract

5-Aminopyrazol-4-yl ketones are prepared rapidly and efficiently using microwave dielectric heating from beta-ketonitriles by treatment with N,N'-diphenylformamidine followed by heterocyclocondensation by irradiation with a hydrazine. The inhibitory activity of RO3201195 prepared by this methodology was confirmed in hTERT-immortalized HCA2 and WS dermal fibroblasts at 200nM concentration, both by ELISA and immunoblot assay, and displays excellent kinase selectivity for p38alpha MAPK over the related stress-activated kinase JNK.

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