Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors

Mourad Chioua, Abdelouahid Samadi, Elena Soriano, Olivier Lozach, Laurent Meijer, José Marco-Contelles

Research output: Contribution to journalArticlepeer-review

81 Citations (Scopus)

Abstract

The synthesis and biological evaluation of a number of differently substituted 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives are reported. From the inhibition results on a selection of disease-relevant protein kinases [IC50 (μM) DYRK1A = 11; CDK5 = 0.41; GSK-3 = 1.5] we have observed that 3,6-diamino-4-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (4) constitutes a potential new and simple lead compound in the search of drugs for the treatment of Alzheimer's disease.

Original languageEnglish
Pages (from-to)4566-4569
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number16
DOIs
Publication statusPublished - Aug 15 2009
Externally publishedYes

Keywords

  • 3,6-Diamino-1H-pyrazolo[3,4-b]pyridine-5-carbonitriles
  • Alzheimer's disease
  • CDK5
  • GSK-3
  • Kinase inhibitors
  • Molecular modelling
  • Pyrazolo[3,4-b]pyridines

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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