5-aryl-pyrazolo[3,4-b]pyridazines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3)

J. Witherington, V. Bordas, David Haigh, D.M.B. Hickey, R.J. Ife, A.D. Rawlings, B.P. Slingsby, D.G. Smith, R.W. Ward

Research output: Contribution to journalArticlepeer-review

Abstract

Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4-b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition. Rationalisation of the binding mode suggested participation of a putative structural water molecule, which was subsequently confirmed by X-ray crystallography. (C) 2003 Elsevier Science Ltd. All rights reserved.
Original languageEnglish
Pages (from-to)1581-1584
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume13
Issue number9
DOIs
Publication statusPublished - 05 May 2003

ASJC Scopus subject areas

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

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