1034732-75-6Relevant academic research and scientific papers
Structure-based optimization of potent PDK1 inhibitors
Angiolini, Mauro,Banfi, Patrizia,Casale, Elena,Casuscelli, Francesco,Fiorelli, Claudio,Saccardo, Maria B.,Silvagni, Marco,Zuccotto, Fabio
, p. 4095 - 4099 (2010)
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.
