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 versu
✦ LIBER ✦
Structure-based design of PDK1 inhibitors
✍ Scribed by Anders Poulsen; Stéphanie Blanchard; Chang Kai Soh; Chaiping Lee; Meredith Williams; Haishan Wang; Brian Dymock
- Book ID
- 113496352
- Publisher
- Elsevier Science
- Year
- 2012
- Tongue
- English
- Weight
- 701 KB
- Volume
- 22
- Category
- Article
- ISSN
- 0960-894X
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