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

16 Citations (Scopus)

Abstract

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
Volume20
Issue number14
Early online date8 Jun 2010
DOIs
Publication statusPublished - 15 Jul 2010

Keywords

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

Fingerprint

Dive into the research topics of 'Structure-based optimization of potent PDK1 inhibitors'. Together they form a unique fingerprint.

Cite this