Structure-based optimization of potent PDK1 inhibitors

Mauro Angiolini (Lead / Corresponding author), Patrizia Banfi, Elena Casale, Francesco Casuscelli, Claudio Fiorelli, Maria B. Saccardo, Marco Silvagni, Fabio Zuccotto

Research output: Contribution to journalArticlepeer-review

19 Citations (Scopus)


In this Letter is described the structure-based design of potent dihydro-pyrazoloquinazolines as PDK1 inhibitors. Starting from low potency HTS hits with the aid of X-ray crystallography and modeling, a medicinal chemistry activity was carried out to improve potency versus PDK1 and selectivity versus CDK2 protein kinase.

Original languageEnglish
Pages (from-to)4095-4099
Number of pages5
JournalBioorganic & Medicinal Chemistry Letters
Issue number14
Early online date8 Jun 2010
Publication statusPublished - 15 Jul 2010


  • CDK2
  • Kinase
  • PDK1
  • Scaffold
  • Structure-based drug design

ASJC Scopus subject areas

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


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