Synthesis of pyrazole derivatives, with biological activity in signal transduction therapy

Edina Miklós, Frigyes Wáczek, György Ker, Szabolcs Lányi, László Örfi

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

A potent kinase inhibitor pyrazole derivative, 1,3-di-tert-butyl-N- (4fiuorophenyl)-1,6-dihydroimidazo[4,5-c]pyrazole-5-amine, has been found in Nested Chemical Library (NCL™) during a high throughput screening (HTS) kinase assay. Since the sample had only 91,3% purity, the biochemical assay was followed by the resynthesis of the hit molecule in a purity of 97%. The repeated biochemical assay showed that the purified substance is inactive. It was concluded that the biological activity should be attributed to one or more minor impurities. The mass spectrum of the original chemical sample showed two minor components. These imidazo[4,5-c]pyrazole-5-yl)-amine derivatives have been synthesized for hit validation purposes.

Original languageEnglish
Pages (from-to)75-82
Number of pages8
JournalUPB Scientific Bulletin, Series B: Chemistry and Materials Science
Volume72
Issue number2
Publication statusPublished - Jun 18 2010

Keywords

  • Heterocyclic molecule
  • Kinase inhibitor
  • Pyrazole derivatives

ASJC Scopus subject areas

  • Chemistry(all)
  • Materials Science(all)

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