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 language | English |
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Pages (from-to) | 4095-4099 |
Number of pages | 5 |
Journal | Bioorganic & Medicinal Chemistry Letters |
Volume | 20 |
Issue number | 14 |
Early online date | 8 Jun 2010 |
DOIs | |
Publication status | Published - 15 Jul 2010 |
Keywords
- 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